Division of Drug Discovery Science

783  articles.  
* There may be some overlapped articles listed due to the difference of format.

  1. Shinohara K, Kobayakawa T, Tsuji K, Takamatsu Y, Mitsuya H, Tamamura H: SARS-CoV‑2 Papain-Like Protease Inhibitors Based on Naphthalen-1-ylethanamine and Halogenated Benzene Moieties. ACS omega. 2025.10; 10 (40): 47165-47175. ( PubMed , DOI )

  2. Tsuji K, Kobayakawa T, Higashi-Kuwata N, Ishii T, Shinohara K, Yamamoto R, Miura Y, Wada N, Mitsuya H, Tamamura H: SARS-CoV‑2 Main Protease Inhibitors Containing 5‑Substituted Benzothiazole-2-carbonyl Moieties at the P1' Site and Their Derivatives. ACS omega. 2025.09; 10 (36): 41608-41619. ( PubMed , DOI )

  3. Okamura, K.; Takeda, K.*; Nagaoka, S.; Ogura, C.; Fukamatsu, M.; Degawa, M.; Kagechika, H.; Ohgane, K.; Kamata, R.; Tanatani, A.: Development and mechanistic evaluation of a lithocholic acid derivative as an environmentally safe rodenticide ACS Pharmacol. Transl. Sci. . 2025.08; 8 2474-2481. ( DOI )

  4. Toyomoto M, Kurihara T, Nakagawa T, Inoue A, Kimura R, Kii I, Sawada T, Ogihara T, Nagayasu K, Kishi T, Onogi, Im D, Asada H, Iwata S, Taguchi J, Sumida Y, Yoshida S, Aoki J, Hosoya T, Hagiwara M: Discovery and development of an oral analgesic targeting the α2B adrenoceptor. Proc Natl Acad Sci U S A. 2025.08; 122 (32): e2500006122. ( PubMed , DOI )

  5. Ishida, R.; Zeng, X.; Kurebayashi, N.; Murayama, T.; Mori, S.; Yamamoto, Y.; Kagechika, H. : Development of selective RyR2 inhibitors with a pharmacophore containing parabanic acid skeleton RSC Med. Chem. . 2025.07; 16 3229-3239. ( DOI )

  6. Tsuji K, Kobayakawa T, Bolah P, Nishimura S, Murakami T, Tamamura H: Hybrid Molecules of Small Molecular and Peptidic HIV Fusion Inhibitors. ChemBioChem. 2025.07; 26 (13): e202500230. ( PubMed , DOI )

  7. Kuyama, K.; Takeda, F.; Ikeda, A,; Tanaka, K.; Katagiri, K.; Kawahata, M.; Okada, Y.; Kobayashi, N.; Kagechika, H.; Tanatani, A.: Aromatic layered foldamer based on (cis, cis)-squaramide: Chiral induction and absolute structure Org. Biomol. Chem.. 2025.05; 23 4927-4933. ( DOI )

  8. Kobayakawa T, Arioka M, Yamamoto K, Tsuji K, Tamamura H: Diastereoselective synthesis of (Z)-fluoroalkene dipeptide isosteres utilizing chiral auxiliaries Org Biomol Chem. 2025.05; 23 (18): 4333-4336. ( PubMed , DOI )

  9. Taguchi J, Ohata Y, Akimoto H, Tabuchi H, Igawa K, Tomooka K, Niwa T, Hosoya T: Boronate Formation-Triggered Azide-Alkyne Cycloaddition. Org Lett. 2025.05; 27 (17): 4428-4433. ( PubMed , DOI )

  10. Suzuki S, Umezawa K, Furuie G, Kikuchi M, Nakamura DGM, Fukahori N, Kimura N, Yamakawa M, Niwa T, Umehara T, Hosoya T, Kii I: Temperature vaulting: A method for screening of slow- and tight-binding inhibitors that selectively target kinases in their non-native state. Eur J Med Chem. 2025.05; 295 117789. ( PubMed , DOI )

  11. Hirano, T.; Yasuda, D.; Yamada, T.; Kagechika, H.: Development of Fluorescent Estrogen Receptor Ligands with pH Sensor Functionality Chem. Pharm. Bull.. 2025.04; 73 (4): 412-418. ( DOI )

  12. Kobayakawa T, Yamamoto K, Fukutome A, Arioka M, Tsuji K, Tamamura H: Design and Synthesis of a C2-Symmetric Cyclic Decapeptide and Its Peptidomimetic as Potential Inhibitors against Amyloid-β Aggregation Synlett. 2025.04;

  13. Watanabe K, Uetake Y, Hata M, Kuwano A, Yamamoto R, Yamamoto Y, Kodera M, Kitagishi H, Niwa T, Hosoya T: Red-light Emitting Orthogonally Trireactive Gold Nanoclusters for the Synthesis of Multifunctionalized Nanomaterials. Small. 2025.04; 21 (17): e2408747. ( PubMed , DOI )

  14. Kawabe, H.; Komiyama, T.; Saito, Y.; Okamoto, Y.; Hara, E.; Matsuzaki, K.; Tori, M.; Hanai, R.; Hirota, H.; Gong, X.; Kuroda, C.; Kagechika, H.; Ohsaki, A.: Grandifolins A–D: three 6/6/5 abietane diterpenes and an abietane diterpene from Salvia grandifolia. J. Nat. Med. . 2025.03; 89 (3): 647-655. ( DOI )

  15. Higashi-Kuwata N, Bulut H, Hayashi H, Tsuji K, Ogata-Aoki H, Kiso M, Takamune N, Kishimoto N, Hattori SI, Ishii T, Kobayakawa T, Nakano K, Shimizu Y, Das D, Saruwatari J, Hasegawa K, Murayama K, Sukenaga Y, Takamatsu Y, Yoshimura K, Aoki M, Furusawa Y, Okamura T, Yamayoshi S, Kawaoka Y, Misumi S, Tamamura H, Mitsuya H: An orally available P1'-5-fluorinated M(pro) inhibitor blocks SARS-CoV-2 replication without booster and exhibits high genetic barrier. PNAS nexus. 2025.01; 4 (1): pgae578. ( PubMed , DOI )

  16. Tanaka T, Tabata S, Nakamura K, Hazama Y, Sakata Y, Hosoya T, Yoshida S: Synthesis of Multisubstituted Naphthalenes through Consecutive Aryne Reactions. Bull Chem Soc Jpn. 2025.01; 98 (1): uoaf001 . ( DOI )

  17. Taguchi J, Omoto Y, Uto K, Uekusa H, Niwa T, Hosoya T: Revisiting the Synthetic Utility of 4,5-Dehydro[2.2]paracyclophane. Adv Synth Catal. 2025.01; 367 (2): e202400986 . ( DOI )

  1. Taguchi J, Tokunaga K, Tabuchi H, Nishiyama T, Kii I, Hosoya T: 1,3-Butadiynyl sulfide-based compact trialkyne platform molecule for sequential assembly of three azides. Chem Commun. 2024.12; 60 (98): 14581-14584. ( PubMed , DOI )

  2. Shinohara K, Kobayakawa T, Tsuji K, Takamatsu Y, Mitsuya H, Tamamura H: Naphthalen-1-ylethanamine-containing small molecule inhibitors of the papain-like protease of SARS-CoV-2. European journal of medicinal chemistry. 2024.12; 280 116963. ( PubMed , DOI )

  3. Tsuji K, Tamamura H, Burke TR: Fine-tuning probes for fluorescence polarization binding assays of bivalent ligands against polo-like kinase 1 using full-length protein. Bioorganic & medicinal chemistry. 2024.12; 119 118055. ( PubMed , DOI )

  4. Kimura, S.; Takeda, F.; Ikeda, A,; Tanimoto, A.; Katagiri, K.; Kawahata, M.; Okada, Y.; Kobayashi, N.; Kagechika, H.; Tanatani, A.: Acid-induced conformational switching of helical foldamers containing imidazole amide. Bull. Chem. Soc. Jpn. 2024.09; 97 (9): uoae094. ( DOI )

  5. Hattori SI, Bulut H, Hayashi H, Kishimoto N, Takamune N, Hasegawa K, Furusawa Y, Yamayoshi S, Murayama K, Tamamura H, Li M, Wlodawer A, Kawaoka Y, Misumi S, Mitsuya H: Structural and virologic mechanism of the emergence of resistance to Mpro inhibitors in SARS-CoV-2 Proc. Natl. Acad. Sci. USA. 2024.09; 121 (37):

  6. Kobayakawa, T; Azuma, C; Yamamoto, K; Tsuji, K; Tamamura, H: | Convergent synthesis of peptidomimetic based on a chloroalkene dipeptide isostere and its application to inhibition against amyloid ß aggregation JOURNAL OF PEPTIDE SCIENCE. 2024.08; 30

  7. Tamamura, H; Higashi-Kuwata, N; Mitsuya, H; Tsuji, K; Ishii, T; Kobayakawa, T: Prevention of the spread of virus infection in global societies: anti-SARS-CoV-2 agents learned from HIV researches JOURNAL OF PEPTIDE SCIENCE. 2024.08; 30

  8. Kobayakawa T, Tsuji K, Tamamura H: Design, synthesis and evaluation of bioactivity of peptidomimetics based on chloroalkene dipeptide isosteres. Bioorganic & medicinal chemistry. 2024.08; 110 117811. ( PubMed , DOI )

  9. Kobayakawa T, Tsuji K, Tamamura H: Design, synthesis and evaluation of bioactivity of peptidomimetics based on chloroalkene dipeptide isosteres. Bioorganic & medicinal chemistry. 2024.08; 110 117811.

  10. Yamashita Yasunobu, Itoh Yukihiro, Takada Yuri, Suzuki Takayoshi: アルツハイマー病治療薬としてのエピジェネティック阻害薬(Frontiers in Alzheimer's and Dementia Research　Epigenetic Inhibitors as Alzheimer's Disease Therapeutic Agents) Chemical & Pharmaceutical Bulletin. 2024.07; 72 (7): 630-637. ( ichushi )

  11. Iida Tetsuya, Itoh Yukihiro, Takahashi Yukari, Miyake Yuka, Zamani Farzad, Yamashita Yasunobu, Takada Yuri, Akiyama Toshiki, Ibaraki Jun, Okuda Kyoka, Tokuda Yuto, Nishimura Tomoka, Hidaka Koto, Mori Hiiro, Oba Makoto, Suzuki Takayoshi: リジンデメチラーゼ5に対する蛋白質分解標的キメラ(PROTAC)の同定とその神経突起伸展促進活性(Frontiers in Alzheimer's and Dementia Research　Identification of Proteolysis Targeting Chimeras(PROTACs) for Lysine Demethylase 5 and Their Neurite Outgrowth-Promoting Activity) Chemical & Pharmaceutical Bulletin. 2024.07; 72 (7): 638-647. ( ichushi )

  12. Tsuji K, Tamamura H, Burke TR Jr: Affinity enhancement of polo-like kinase 1 polo box domain-binding ligands by a bivalent approach using a covalent kinase-binding component. RSC chemical biology. 2024.07; 5 (8): 721-728. ( PubMed , DOI )

  13. Tsuji Kohei, Tamamura Hirokazu, Burke Jr. Terrence R.: Polo like kinase 2とpolo like kinase 3に対する蛍光回復に基づくポロ様キナーゼ1の結合測定法の応用(Application of a Fluorescence Recovery-Based Polo-Like Kinase 1 Binding Assay to Polo-Like Kinase 2 and Polo-Like Kinase 3) Biological & Pharmaceutical Bulletin. 2024.07; 47 (7): 1282-1287. ( ichushi )

  14. Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule. 2024.06; 105 129759. ( PubMed , DOI )

  15. Ishii T, Kobayakawa T, Matsuda K, Nigorikawa K, Bolah P, Noborio A, Tsuji K, Ohashi N, Yoshimura K, Nomura W, Mitsuya H, Maeda K, Tamamura H: Discovery of Potent DAG-Lactone Derivatives as HIV Latency Reversing Agents. ACS infectious diseases. 2024.05; 10 (6): 2250-2261. ( PubMed , DOI )

  16. Shiino H, Tashiro S, Hashimoto M, Sakata Y, Hosoya T, Endo T, Kojima H, Tamura Y: Chemical inhibition of phosphatidylcholine biogenesis reveals its role in mitochondrial division. iScience. 2024.03; 27 (3): 109189. ( PubMed , DOI )

  17. Nurani Atika, Yamashita Yasunobu, Taki Yuuki, Takada Yuri, Itoh Yukihiro, Suzuki Takayoshi: 機械学習を基盤とした薬物スクリーニングを介したヒストン脱アセチル化酵素8阻害剤の同定(Advanced Medicinal Chemistry in Academia　Identification of a Histone Deacetylase 8 Inhibitor through Drug Screenings Based on Machine Learning) Chemical & Pharmaceutical Bulletin. 2024.02; 72 (2): 173-178. ( ichushi )

  18. Takada Yuri, Adachi Kyohei, Fujinaga Yuka, Yamashita Yasunobu, Itoh Yukihiro, Suzuki Takayoshi: リジン特異的脱メチル化酵素1阻害剤としてのSNAIL1ペプチドの構造活性相関研究(Advanced Medicinal Chemistry in Academia　A Structure-Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1) Chemical & Pharmaceutical Bulletin. 2024.02; 72 (2): 155-160. ( ichushi )

  19. Design, synthesis, and biological evaluation of phenylcyclopropylamine-entinostat conjugates that selectively target cancer cells. 2024.02; 100 117632. ( PubMed , DOI )

  20. Structural optimization of a lysine demethylase 5 inhibitor for improvement of its cellular activity. 2024.01; 98 117579. ( PubMed , DOI )

  21. Discrete prefrontal neuronal circuits determine repeated stress-induced behavioral phenotypes in male mice. 2024.01; ( PubMed , DOI )

  22. Watanabe K, Mao Q, Zhang Z, Hata M, Kodera M, Kitagishi H, Niwa T, Hosoya T: Clickable bisreactive small gold nanoclusters for preparing multifunctionalized nanomaterials: application to photouncaging of an anticancer molecule. Chem Sci. 2024.01; 15 (4): 1402-1408. ( PubMed , DOI )

  23. Kobayakawa Takuya, Yokoyama Masaru, Tsuji Kohei, Boku Sayaka, Kurakami Masaki, Fujino Masayuki, Ishii Takahiro, Miura Yutaro, Nishimura Soshi, Shinohara Kouki, Yamamoto Kenichi, Bolah Peter, Kotani Osamu, Murakami Tsutomu, Sato Hironori, Tamamura Hirokazu: Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins(タイトル和訳中) Chemical & Pharmaceutical Bulletin. 2024.01; 72 (1): 41-47. ( ichushi )

  24. Kobayakawa T, Yokoyama M, Tsuji K, Boku S, Kurakami M, Fujino M, Ishii T, Miura Y, Nishimura S, Shinohara K, Yamamoto K, Bolah P, Kotani O, Murakami T, Sato H, Tamamura H: Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins. Chemical & pharmaceutical bulletin. 2024; 72 (1): 41-47. ( PubMed , DOI )

  25. Tsuji K, Tamamura H, Burke TR Jr: Application of a Fluorescence Recovery-Based Polo-Like Kinase 1 Binding Assay to Polo-Like Kinase 2 and Polo-Like Kinase 3. Biological & pharmaceutical bulletin. 2024; 47 (7): 1282-1287. ( PubMed , DOI )

  26. Epigenetic Inhibitors as Alzheimer's Disease Therapeutic Agents. 2024; 72 (7): 630-637. ( PubMed , DOI )

  27. Identification of a Histone Deacetylase 8 Inhibitor through Drug Screenings Based on Machine Learning. 2024; 72 (2): 173-178. ( PubMed , DOI )

  28. A Structure-Activity Relationship Study of SNAIL1 Peptides as Inhibitors of Lysine-Specific Demethylase 1. 2024; 72 (2): 155-160. ( PubMed , DOI )

  29. Ishida R, Zeng X, Kurebayashi N, Murayama T, Mori S, Kagechika H: Discovery and Structure-Activity Relationship of a Ryanodine Receptor 2 Inhibitor. Chemical & pharmaceutical bulletin. 2024; 72 (4): 399-407. ( PubMed , DOI )

  30. Kobayakawa T, Takano H, Ishii T, Bolah P, Tsuji K, Ohashi N, Nomura W, Furuta T, Tamamura H: Effect of Two-Photon Excitation to 8-Azacoumarin Derivatives as Photolabile Protecting Groups. Chemical & pharmaceutical bulletin. 2024; 72 (3): 311-312. ( PubMed , DOI )

  1. Kohei Tsuji, Takuya Kobayakawa, Takahiro Ishii, Nobuyo Higashi-Kuwata, Chika Azuma, Kouki Shinohara, Yutaro Miura, Kenichi Yamamoto, Soshi Nishimura, Shin-ichiro Hattori, Haydar Bulut, Hiroaki Mitsuya, Hirokazu Tamamura: Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement. Chemical and Pharmaceutical Bulletin. 2023.12; 71 (12): 879-886. ( PubMed , DOI )

  2. Takenaka, M.; Kodama, M.; Murayama, T.; Ishigami-Yuasa, M.; Mori, S.; Ishida, R.; Suzuki, J.; Kanemaru, K.; Sugihara, M.; Iino, M.; Miura, A.; Nishio, H.; Morimoto, S.; Kagechika, H.; Sakurai, T.; Kurebayashi, N.: Screening for novel Ryanodine Receptor inhibitors by Endoplasmic Reticulum Ca2+ monitoring Mol. Pharmacol.. 2023.12; 104 275-286. ( DOI )

  3. Tsuji Kohei, Kobayakawa Takuya, Ishii Takahiro, Higashi-Kuwata Nobuyo, Azuma Chika, Shinohara Kouki, Miura Yutaro, Yamamoto Kenichi, Nishimura Soshi, Hattori Shin-ichiro, Bulut Haydar, Mitsuya Hiroaki, Tamamura Hirokazu: Exploratory Studies of Effective Inhibitors against the SARS-CoV-2 Main Protease by Halogen Incorporation and Amide Bond Replacement(タイトル和訳中) Chemical & Pharmaceutical Bulletin. 2023.12; 71 (12): 879-886. ( ichushi )

  4. Ishida R, Kurebayashi N, Iinuma H, Zeng X, Mori S, Kodama M, Murayama T, Masuno H, Takeda F, Kawahata M, Tanatani A, Miura A, Nishio H, Sakurai T, Kagechika H: A potent and selective cis-amide inhibitor of ryanodine receptor 2 as a candidate for cardiac arrhythmia treatment. European journal of medicinal chemistry. 2023.12; 262 115910. ( PubMed , DOI )

  5. Niwa T, Takimoto T, Sakata Y, Hosoya T: Palladium-Catalyzed #Iipso#IR-Borylation of Aryl Halides Promoted by Lewis Acid-Mediated Electrophilic Activation of Aryl(halo)palladium(II) Complex. Org Lett. 2023.11; 25 (45): 8173-8177. ( PubMed , DOI )

  6. Nakanishi, S.; Kinoshita, K.; Kurauchi, Y.; Seki, T.; Kimura, Y.; Suzuki, M.; Suzuki, K.; Koyama, H.; Kagechika, H.; Katsuki, H.: Acyclic retinoid peretinoin reduces hemorrhage-associated brain injury in vitro and in vivo Eur. J. Pharmacol.. 2023.09; 954 175899. ( DOI )

  7. Tsuji K, Ishii T, Kobayakawa T, Higashi-Kuwata N, Shinohara K, Azuma C, Miura Y, Nakano H, Wada N, Hattori SI, Bulut H, Mitsuya H, Tamamura H: Structure-Activity Relationship Studies of SARS-CoV-2 Main Protease Inhibitors Containing 4-Fluorobenzothiazole-2-carbonyl Moieties. Journal of medicinal chemistry. 2023.09; 66 (19): 13516-13529. ( PubMed , DOI )

  8. Taguchi J, Okuyama T, Tomita S, Niwa T, Hosoya T: Synthesis of Multisubstituted Aromatics via 3-Triazenylarynes. Org Lett. 2023.09; 25 (38): 7030-7034. ( PubMed , DOI )

  9. Tanaka.; Takeda, F.; Kanda, M.; Kawahata,M.; Fujii,S.; Katagiri,K.; Masu, H.; Kagechika,H.; Tanatani, A.: Solvent-Dependent Conformational Switching of N-Methyl-N,N'- diarylsquaramide J. Org. Chem.. 2023.08; 88 12289-12293. ( DOI )

  10. Takahiro Ishii, Takuya Kobayakawa, Kouki Matsuda, Kohei Tsuji, Nami Ohashi, Shingo Nakahata, Airi Noborio, Kazuhisa Yoshimura, Hiroaki Mitsuya, Kenji Maeda, Hirokazu Tamamura: Synthesis and evaluation of DAG-lactone derivatives with HIV-1 latency reversing activity. European Journal of Medicinal Chemistry. 2023.08; 256 115449. ( PubMed , DOI )

  11. Mansell, J. P.; Tanatani, A.; Kagechika, H.: An N-cyanoamide derivative of lithocholic acid co-operates with lysophosphatidic acid to promote human osteoblast (MG63) differentiation Biomolecules. 2023.07; 13 1113. ( DOI )

  12. Zhang Z, Niwa T, Watanabe K, Hosoya T: #U11#URC-Cyanation of Aryl Fluorides via Nickel and Lithium Chloride-Mediated C-F Bond Activation. Angew Chem Int Ed Engl. 2023.05; 62 (22): e202302956. ( PubMed , DOI )

  13. Origin of the kinetic HDAC2 ‐selectivity of an HDAC inhibitor 2023.04; 44 (18): 1604-1609. ( PubMed , DOI )

  14. Nhieu, J.; Milbauer, L.; Lerdall, T.; Najjar, F.; Wei, C.-W.; Ishida, R.; Ma, Y.; Kagechika, H.; Wei, L.-N.: Targeting Cellular Retinoic Acid Binding Protein 1 with Retinoic Acid-like Compounds to Mitigate Motor Neuron Degeneration Int. J. Mol. Sci.. 2023.03; 24 4980.

  15. Niwa T, Tahara T, Chase CE, Fang FG, Nakaoka T, Irie S, Hayashinaka E, Wada Y, Mukai H, Masutomi K, Watanabe Y, Cui Y, Hosoya T: Synthesis of #U11#URC-Radiolabeled Eribulin as a Companion Diagnostics PET Tracer for Brain Glioblastoma. Bull Chem Soc Jpn. 2023.03; 96 (3): 283-290. ( DOI )

  16. Dubol M, Immenschuh J, Jonasson M, Takahashi K, Niwa T, Hosoya T, Roslin S, Wikström J, Antoni G, Watanabe Y, Lubberink M, Biegon A, Sundström-Poromaa I, Comasco E: Acute nicotine exposure blocks aromatase in the limbic brain of healthy women: A [#U11#URC]cetrozole PET study. Compr Psychiatry. 2023.03; 123 152381. ( PubMed , DOI )

  17. Kohei Tsuji, Kofi Baffour-Awuah Owusu, Yutaro Miura, Takahiro Ishii, Kouki Shinohara, Takuya Kobayakawa, Akino Emi, Takashi Nakano, Youichi Suzuki, Hirokazu Tamamura : Dimerized fusion inhibitor peptides targeting the HR1–HR2 interaction of SARS-CoV-2 RSC Advances. 2023.03; 13 8779-8793.

  18. Sakata Y, Nabekura R, Hazama Y, Hanya M, Nishiyama T, Kii I, Hosoya T: Synthesis of Functionalized Dibenzoazacyclooctynes by a Decomplexation Method for Dibenzo-Fused Cyclooctyne-Cobalt Complexes. Org Lett. 2023.02; 25 (7): 1051-1055. ( PubMed , DOI )

  19. Tabata S, Minoshima M, Kobayashi A, Matsuzawa T, Hosoya T, Yoshida S: Migrative Thioamination of Aryne Intermediates Generated from #Io#IR-Iodoaryl Triflates. Synlett. 2023.02; ( DOI )

  20. Higashi-Kuwata N, Tsuji K, Hayashi H, Bulut H, Kiso M, Imai M, Ogata-Aoki H, Ishii T, Kobayakawa T, Nakano K, Takamune N, Kishimoto N, Hattori SI, Das D, Uemura Y, Shimizu Y, Aoki M, Hasegawa K, Suzuki S, Nishiyama A, Saruwatari J, Shimizu Y, Sukenaga Y, Takamatsu Y, Tsuchiya K, Maeda K, Yoshimura K, Iida S, Ozono S, Suzuki T, Okamura T, Misumi S, Kawaoka Y, Tamamura H, Mitsuya H: Identification of SARS-CoV-2 M(pro) inhibitors containing P1' 4-fluorobenzothiazole moiety highly active against SARS-CoV-2. Nature communications. 2023.02; 14 (1): 1076. ( PubMed , DOI )

  21. Kobayashi A, Matsuzawa T, Hosoya T, Yoshida S: Synthesis of benzo[#Ib#IR]furans from alkynyl sulfoxides and phenols by the interrupted Pummerer reaction. RSC Adv. 2023.01; 13 (2): 839-843. ( PubMed , DOI )

  22. Kitamura H., Sukegawa S., Matsuda K., Tanimoto K., Kobayakawa T., Takahashi K., Tamamura H., Tsuchiya K., Gatanaga H., Maeda K., and Takeuchi H.: 4-phenylquinoline-8-amine induces HIV-1 reactivation and apoptosis in latently HIV-1 infected cells. Biochemical and Biophysical Research Communications. 2023.01; 641 139-147. ( PubMed , DOI )

  1. Tsuboi, Y.; Oyama, K.; Kobirumaki-Shimozawa, F.; Murayama, T.; Kurebayashi, N.; Tachibana, T.; Manome, Y.; Kikuchi, E.; Noguchi, S.; Inoue, T.; Inoue, Y. U.; Nishino, I.; Mori, S.; Ishida, R.; Kagechika, H.; Suzuki, M.; Fukuda, N.; Yamazawa, T.: Mice with R2509C-RYR1 mutation exhibit dysfunctional Ca2+ dynamics in primary skeletal myocytes J. Gen. Physiol.. 2022.12; 154 e202213136.

  2. Rongyi Wang, Kohei Tsuji, Takuya Kobayakawa, Yishan Liu, Kazuhisa Yoshimura, Shuzo Matsushita, Shigeyoshi Harada, Hirokazu Tamamura: Hybrids of small CD4 mimics and gp41-related peptides as dual-target HIV entry inhibitors Bioorganic & Medicinal Chemistry. 2022.12; 76 117083. ( PubMed , DOI )

  3. Matsuura K, Yamaura M, Sakawaki H, Himeno A, Pisil Y, Kobayakawa T, Tsuji K, Tamamura H, Matsushita S, Miura T: Sensitivity to a CD4 mimic of a consensus clone of monkey-adapted CCR5-tropic SHIV-MK38C. Virology. 2022.12; 578 171-179. ( PubMed , DOI )

  4. Murayama, T.; Kurebayashi, N.; Numaga-Tomita, T.; Kobayashi, T.; Okazaki, S.; Yamashiro, K.; Nakada, T.; Mori, S.; Ishida, R.; Kagechika, H.; Yamada, M.; Sakurai, T.: A reconstituted depolarization-induced Ca2+ release platform for validation of skeletal muscle disease mutations and drug discovery. J. Gen. Physiol.. 2022.12; 154 (12): e202213230. ( DOI )

  5. Matsumoto K, Kuwata T, Tolbert WD, Richard J, Ding S, Prévost J, Takahama S, Judicate GP, Ueno T, Nakata H, Kobayakawa T, Tsuji K, Tamamura H, Smith AB 3rd, Pazgier M, Finzi A, Matsushita S: Characterization of a Novel CD4 Mimetic Compound YIR-821 against HIV-1 Clinical Isolates. Journal of virology. 2022.12; 97 (1): e0163822. ( PubMed , DOI )

  6. Yamada, S.; Masuno, H.; Kagechika, H.; Tanatani, A.; Kanda, Y: A Novel Lithocholic Acid Derivative Upregulates Detoxification-Related Genes in Human Induced Pluripotent Stem Cell-Derived Intestinal Organoids. Biol. Pharm. Bull.. 2022.11; 45 (1720): 1724.

  7. Tsuji K, Ishii T, Kobayakawa T, Higashi-Kuwata N, Azuma C, Nakayama M, Onishi T, Nakano H, Wada N, Hori M, Shinohara K, Miura Y, Kawada T, Hayashi H, Hattori SI, Bulut H, Das D, Takamune N, Kishimoto N, Saruwatari J, Okamura T, Nakano K, Misumi S, Mitsuya H, Tamamura H: Potent and biostable inhibitors of the main protease of SARS-CoV-2. iScience. 2022.11; 105365. ( PubMed , DOI )

  8. Tsuji K, Ishii T, Kobayakawa T, Higashi-Kuwata N, Azuma C, Nakayama M, Onishi T, Nakano H, Wada N, Hori M, Shinohara K, Miura Y, Kawada T, Hayashi H, Hattori SI, Bulut H, Das D, Takamune N, Kishimoto N, Saruwatari J, Okamura T, Nakano K, Misumi S, Mitsuya H, Tamamura H: Potent and biostable inhibitors of the main protease of SARS-CoV-2. iScience. 2022.11; 105365. ( PubMed , DOI )

  9. Katayama A, Jin Y, Nishiyama Y, Hosoya T, Yokoshima S: Substitution of α-Azido Sulfones with Thiolates to Form α-Azido Sulfides. Org Lett. 2022.10; 24 (40): 7361-7365. ( PubMed , DOI )

  10. Cancer-Cell-Selective Targeting by Arylcyclopropylamine-Vorinostat Conjugates. 2022.10; 13 (10): 1568-1573. ( PubMed , DOI )

  11. Zhe Wei, Hoshina Naomi, Itoh Yukihiro, Tojo Toshifumi, Suzuki Takayoshi, Hase Koji, Takahashi Daisuke: 新規HDAC1選択的阻害薬は炎症性サイトカイン産生阻害により自己免疫性関節炎を軽減する(A Novel HDAC1-Selective Inhibitor Attenuates Autoimmune Arthritis by Inhibiting Inflammatory Cytokine Production) Biological & Pharmaceutical Bulletin. 2022.09; 45 (9): 1364-1372. ( ichushi )

  12. Takubo, C.; Kimura, S.; Ichinomiya, M.; Hayakawa, A.; Murata, M.; Urushibara, K.; Masu, H.; Katagiri, K.; Kawahata, M.; Kudo, M.; Azumaya, I.; Kagechika, H.; Tanatani, A. : Conformational Properties of Aromatic Amides Bearing Imidazole Ring and Acid-induced trans-cis Amide Switching J. Org. Chem.. 2022.09; 88 16707-16718. ( DOI )

  13. Inouye S, Sato J, Sahara-Miura Y, Tomabechi Y, Sumida Y, Sekine S, Shirouzu M, Hosoya T: Reverse mutants of the catalytic 19 kDa mutant protein (nanoKAZ/nanoLuc) from #IOplophorus#IR luciferase with coelenterazine as preferred substrate. PLoS One. 2022.09; 17 (9): e0272992. ( PubMed , DOI )

  14. Ishida, R.; Mori, S.; Murayama, T.; Nakamichi, A.; Chai, X.; Kurebayashi, N. Iinuma, H.; Kagechika, H.: Development of a water-soluble ryanodine receptor 1 inhibitor. Bioorg. Med. Chem.. 2022.09; 74 117027. ( DOI )

  15. Watanabe K, Kuratsu A, Hashizume D, Niwa T, Hosoya T: Red light-induced conjugation of amines through amide bond formation triggered via photooxidation of 3-acylindolizines. Commun Chem. 2022.08; 5 (1): 91. ( PubMed , DOI )

  16. Mori, S.; Tsuemoto, N.; Kawachi, E.; Takubo, C.; Tanatani, A.; Kagechika, H.: Development of retinoic acid receptor antagonists bearing trans-SF4-alkynyl structure as a linear linker. Tetrahedron . 2022.08; 123 132967. ( DOI )

  17. Kohei Tsuji, David Hymel, Buyong Ma, Hirokazu Tamamura, Ruth Nussinov, Terrence R Burke Jr: Development of ultra-high affinity bivalent ligands targeting the polo-like kinase 1. RSC chemical biology. 2022.08; 3 (9): 1111-1120. ( PubMed , DOI )

  18. Hara Y, Ando F, Oikawa D, Ichimura K, Yanagawa H, Sakamaki Y, Nanamatsu A, Fujiki T, Mori S, Suzuki S, Yui N, Mandai S, Susa K, Mori T, Sohara E, Rai T, Takahashi M, Sasaki S, Kagechika H, Tokunaga F, Uchida S: LRBA is essential for urinary concentration and body water homeostasis. Proceedings of the National Academy of Sciences of the United States of America. 2022.07; 119 (30): e2202125119. ( PubMed , DOI )

  19. Hara, Y.; Ando, F.; Oikawa, D.; Ichimura, K.; Yanagawa, H.; Sakamaki, Y.; Nanamatsu, A.; Fujiki, T.; Mori, S.; Suzuki, S.; Yui, N.; Mandai, S.; Susa, K.; Mori, T.; Sohara, E.; Rai, T.; Takahashi, M.; Sasaki, S.; Kagechika, H.; Tokunaga, F.; Uchida, S.: LRBA is essential for urinary concentration and body water homeostasis Proc. Natl. Acad. Sci. USA. 2022.07; 119 (30): e2202125119.

  20. Oikawa, T.; Fujii, S.; Mori, S.; Masuno, H.; Kawachi, E.; Kagechika, H. : Structural Development of Silicon-Containing Retinoids: Structure–Activity Relationship Study of the Hydrophobic Pharmacophore of Retinobenzoic Acids Using Silyl Functionalities ChemMedChem. 2022.06; e202200176.

  21. Sugiyama K, Sakata Y, Niwa T, Yoshida S, Hosoya T: Azido-type-selective triazole formation by iridium-catalyzed cycloaddition with thioalkynes. Chem Commun. 2022.05; 58 (42): 6235-6238. ( PubMed , DOI )

  22. Recent progress on small molecules targeting epigenetic complexes. 2022.04; 67 102130. ( PubMed , DOI )

  23. Nagai A, Kobayashi A, Sakata Y, Minami Y, Uchida K, Hosoya T, Yoshida S: Synthesis of Multisubstituted Benzenes from Phenols via Multisubstituted Benzynes. Synthesis. 2022.04; 54 (22): 5017-5025. ( DOI )

  24. Fukuchi T, Niwa T, Hosoya T, Watanabe Y: Computational study for amino acid production from carboxylic acid #Ivia#IR #U14#URC β-decay. J Phys Soc Jpn. 2022.04; 91 (6): 064301. ( DOI )

  25. Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC). 2022.03; 58 (29): 4635-4638. ( PubMed , DOI )

  26. Kimura N, Saito K, Niwa T, Yamanaka M, Igaue S, Ohkanda J, Hosoya T, Kii I: Expression and purification of DYRK1A kinase domain in complex with its folding intermediate-selective inhibitor FINDY. Protein Expres Purif. 2022.03;

  27. Idogawa R, Kobayashi A, Kim Y, Shimomori K, Hosoya T, Yoshida S: Hydride reduction of #Io#IR-(fluorosilyl)benzodifluorides for subsequent C-F transformations. Chem Commun. 2022.03; 58 (21): 3521-3524. ( PubMed , DOI )

  28. Nakaoka T, Kaneko K, Irie S, Mawatari A, Igesaka A, Uetake Y, Ochiai H, Niwa T, Yamano E, Wada Y, Tanaka M, Kotani K, Kawahata H, Kawabe J, Miki Y, Doi H, Hosoya T, Maeda K, Kusuhara H, Sugiyama Y, Watanabe Y: Clinical evaluation of [#U18#URF]pitavastatin for quantitative analysis of hepatobiliary transporter activity. Drug Metab Pharmacok. 2022.02; ( DOI )

  29. Takemura H, Orimoto G, Kobayashi A, Hosoya T, Yoshida S: Modular synthesis of triazoles from 2-azidoacrylamides having a nucleophilic amino group. Org Biomol Chem. 2022.02; ( PubMed , DOI )

  30. Tsuji K, Kobayakawa T, Konno K, Masuda A, Takahashi K, Ohashi N, Yoshimura K, Kuwata T, Matsushita S, Harada S, Tamamura H: Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors. Bioorganic & medicinal chemistry. 2022.01; 56 116616. ( PubMed , DOI )

  31. Inouye S, Nakamura M, Hosoya T: Enzymatic conversion of dehydrocoelenterazine to coelenterazine using FMN-bound flavin reductase of NAD(P)H:FMN oxidoreductase. Biochem Biophys Res Commun. 2022.01; 587 24-28. ( PubMed , DOI )

  32. Miyazaki Y, Kikuchi M, Umezawa K, Descamps A, Nakamura D, Furuie G, Sumida T, Saito K, Kimura N, Niwa T, Sumida Y, Umehara T, Hosoya T, Kii I: Structure-activity relationship for the folding intermediate-selective inhibition of DYRK1A. Eur J Med Chem. 2022.01; 227 113948. ( PubMed , DOI )

  33. Yoshihara, A.; Kawasaki, H.; Masuno, M.; Takada, K.; Numoto, N.; Ito, N.; Hirata, N.; Kanda, Y.; Ishizawa, M.; Makishima, M.; Kagechika, H.; Tanatani, A.: Lithocholic Acid Amides as Potent Vitamin D Receptor Agonists Biomolecules. 2022.01; 12 (1): 130.

  34. Yoshihara Ayana, Kawasaki Haru, Masuno Hiroyuki, Takada Koki, Numoto Nobutaka, Ito Nobutoshi, Hirata Naoya, Kanda Yasunari, Ishizawa Michiyasu, Makishima Makoto, Kagechika Hiroyuki, Tanatani Aya: Lithocholic Acid Amides as Potent Vitamin D Receptor Agonists BIOMOLECULES. 2022.01; 12 (1): ( PubMed , DOI )

  35. A Novel HDAC1-Selective Inhibitor Attenuates Autoimmune Arthritis by Inhibiting Inflammatory Cytokine Production. 2022; 45 (9): 1364-1372. ( PubMed , DOI )

  1. Takahashi K, Hosoya T, Onoe K, Mori T, Tazawa S, Mawatari A, Wada Y, Watanabe Y, Doi H, Watanabe Y: PET imaging of brain aromatase in humans and rhesus monkeys by #U11#URC-labeled cetrozole analogs. Sci Rep. 2021.12; 11 (1): 23623. ( PubMed , DOI )

  2. Niwa T, Uetake Y, Isoda M, Takimoto T, Nakaoka M, Hashizume D, Sakurai H, Hosoya T: Lewis acid-mediated Suzuki–Miyaura cross-coupling reaction. Nat Catal. 2021.12; 4 (12): 1080-1088. ( DOI )

  3. Inouye S, Nakamura M, Hosoya T: Formation of Coelenteramine from 2-Peroxycoelenterazine in the Ca#U2+#UR-Binding Photoprotein Aequorin. Photochem Photobiol. 2021.12; ( PubMed , DOI )

  4. Sakata Y, Yoshida S, Hosoya T: Synthesis of Azidoanilines by the Buchwald-Hartwig Amination. J Org Chem. 2021.11; 86 (21): 15674-15688. ( PubMed , DOI )

  5. Taguchi J, Kimura K, Igawa K, Tomooka K, Hosoya T: 3-Azidoarynes: Generation and Regioselective Reactions. Chem Lett. 2021.11; 51 (2): 94-98. ( DOI )

  6. Identification of Potent and Selective Inhibitors of Fat Mass Obesity-Associated Protein Using a Fragment-Merging Approach. 2021.11; 64 (21): 15810-15824. ( PubMed , DOI )

  7. Takayanagi, S.; Watanabe, K.; Maruyama, T.; Ogawa, M.; Morishita, K.; Soga, M.; Hatta, T.; Natsume, T.; Hirano, T.; Kagechika, H.; Hattori, K.; Naguro, I.; Ichijo, H.: ASKA technology-based pull-down method reveals a suppressive effect of ASK1 on the inflammatory NOD-RIPK2 pathway in brown adipocytes Sci. Rep.. 2021.10; 11 22009.

  8. Kohei Tsuji, Takahiro Ishii, Takuya Kobayakawa, Nami Ohashi, Wataru Nomura & Hirokazu Tamamura: Fluorescence resonance energy transfer-based screening for protein kinase C ligands using 6-methoxynaphthalene-labeled 1,2-diacylglycerol-lactones. Organic & Biomolecular Chemistry. 2021.10; 19 (38): 8264-8271. ( PubMed , DOI )

  9. Watanabe K, Terao N, Niwa T, Hosoya T: Direct 3-Acylation of Indolizines by Carboxylic Acids for the Practical Synthesis of Red Light-Releasable Caged Carboxylic Acids. J Org Chem. 2021.09; 86 (17): 11822-11834. ( PubMed , DOI )

  10. Fujii, S.; Kikuchi, E.; Suzuyama, H.; Watanabe, Y.; Ishigami-Yuasa, M.; Masuno, H.; Mori, T.; Isobe, K.; Uchida, S.; Kagechika, H.: Structural Development of Salicylanilide-Based SPAK Inhibitors as Candidate Antihypertensive Agents ChemMedChem. 2021.09; 16 (18): 2817-2822.

  11. David Hymel, Kohei Tsuji, Robert A Grant, Ramesh M Chingle, Dominique L Kunciw, Michael B Yaffe, Terrence R Burke Jr: Design and synthesis of a new orthogonally protected glutamic acid analog and its use in the preparation of high affinity polo-like kinase 1 polo-box domain - binding peptide macrocycles. Organic & Biomolecular Chemistry. 2021.09; 19 (36): 7843-7854. ( PubMed , DOI )

  12. Hasan Md Zahid, Takeo Kuwata, Shokichi Takahama, Yu Kaku, Shashwata Biswas, Kaho Matsumoto, Hirokazu Tamamura & Shuzo Matsushita: Functional Analysis of a Monoclonal Antibody Reactive against the C1C2 of Env Obtained from a Patient Infected with HIV-1 CRF02_AG. Retrovirology. 2021.08; 18 (1): 23(article number).

  13. Lin Liu, Hiroyuki Koike, Takehito Ono, Shinichiro Hayashi, Fujimi Kudo, Atsushi Kaneda, Hiroyuki Kagechika, Ichiro Manabe, Tomoki Nakashima, Yumiko Oishi: Identification of a KLF5-dependent program and drug development for skeletal muscle atrophy. Proc Natl Acad Sci U S A. 2021.08; 118 (35): ( PubMed , DOI )

  14. Fujii Shinya, Kikuchi Eriko, Suzuyama Honoka, Watanabe Yuko, Ishigami-Yuasa Mari, Masuno Hiroyuki, Mori Takayasu, Isobe Kiyoshi, Uchida Shinichi, Kagechika Hiroyuki: Structural Development of Salicylanilide-Based SPAK Inhibitors as Candidate Antihypertensive Agents CHEMMEDCHEM. 2021.07; 16 (18): 2817-2822. ( PubMed , DOI )

  15. Konishi, M.; Noguchi, S.; Inoue, T.; Inoue, Y. U.; Nishino, I.; Mori, S.; Iinuma, H.; Manaka, N.; Kagechika, H.; Uryash, A.; Adams, J.; Lopez, J. R.; Liu, X. C.; Diggle, C.; Allen, P. D.; Kakizawa, S.; Ikeda, K.; Lin, B. Z.; Ikemi, Y.; Nunomura, K.; Nakagawa, S.; Sakurai, T.; Murayama, T.: A novel RyR1-selective inhibitor prevents and rescues sudden death in mouse models of malignant hyperthermia and heat stroke Nature Commun.. 2021.07; 12 (1): 4293. ( DOI )

  16. Identification of Novel Histone Deacetylase 6-Selective Inhibitors Bearing 3,3,3-Trifluorolactic Amide (TFLAM) Motif as a Zinc Binding Group. 2021.07; 22 (22): 3158-3163. ( PubMed , DOI )

  17. Kobayashi K, Matsuzawa T, Hosoya T, Yoshida S: Thioxanthone Synthesis from Benzoic Acid Esters through Directed #Iortho#IR-Lithiation. Chem Lett. 2021.06; 50 (9): 1624-1627. ( DOI )

  18. Aimi T, Meguro T, Kobayashi A, Hosoya T, Yoshida S: Nucleophilic transformations of azido-containing carbonyl compounds via protection of the azido group. Chem Commun. 2021.06; 57 (49): 6062-6065. ( PubMed , DOI )

  19. Lin, Y.-W.; Nhieu, J.; Wei, C.-W.; Lin, Y.-L.; Kagechika, H.; Wei, L.-N.: Regulation of exosome secretion by cellular retinoic acid binding protein 1 contributes to systemic anti-inflammation Cell Commun. Signal.. 2021.06; 19 (1): 69. ( PubMed , DOI )

  20. Kobayashi T, Hosoya T, Yoshida S: Facile Synthetic Methods for Diverse #IN#IR-Arylphenylalanine Derivatives via Transformations of Aryne Intermediates and Cross-Coupling Reactions. Bull Chem Soc Jpn. 2021.05; 94 (7): 1823-1832. ( DOI )

  21. Matsuura, S; Taguchi, J; Seki, T; Ito, H: Synthesis and Optical Properties of C,N-Swapped Boranils Derived from Potassium Acyltrifluoroborates BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN. 2021.05; 94 (5): 1547-1552. ( DOI )

  22. Jan Vincent V. Arafiles, Hisaaki Hirose, Yusuke Hirai, Masashi Kuriyama, Maxwell Mamfe Sakyiamah, Wataru Nomura, Kazuhiro Sonomura, Miki Imanishi, Akira Otaka, Hirokazu Tamamura & Shiroh Futaki: Discovery of a Macropinocytosis-inducing Peptide Potentiated by Medium-mediated Intramolecular Disulfide Formation. Angewandte Chemie International Edition. 2021.05; 60 (21): 11928-11936.

  23. Yoshida S, Hosoya T: Recent Insertion Reactions of Aryne Intermediates. Modern Aryne Chemistry (Ed. Biju AT). 2021.05; 111-148. ( DOI )

  24. Nagashima S, Maruyama J, Honda K, Kondoh Y, Osada H, Nawa M, Nakahama KI, Ishigami-Yuasa M, Kagechika H, Sugimura H, Iwasa H, Arimoto-Matsuzaki K, Nishina H, Hata Y: CSE1L promotes nuclear accumulation of transcriptional coactivator TAZ and enhances invasiveness of human cancer cells. The Journal of biological chemistry. 2021.05; 297 (1): 100803. ( PubMed , DOI )

  25. Kato, D.; Shiraishi, T.; Kagechika, H.; Hirano, T.: Design, synthesis and antitumor activity of phthalazine-1,4-dione-based menaquinone analogs Bioorg. Med. Chem. Lett.. 2021.04; 43 128065. ( PubMed , DOI )

  26. Suzuki M, Kanemoto K, Nakamura Y, Hosoya T, Yoshida S: Palladium-Catalyzed Sulfinylation of Aryl- and Alkenylborons with Sulfinate Esters. Org Lett. 2021.03; 23 (9): 3793-3797. ( PubMed , DOI )

  27. Takuya Kobayakawa, Chika Azuma, Yuki Watanabe, Shunsuke Sawamura, Atsuhiko Taniguchi, Yoshio Hayashi, Kohei Tsuji & Hirokazu Tamamura: Development of Methods for Convergent Synthesis of Chloroalkene Dipeptide Isosteres and Its Application. The Journal of Organic Chemistry. 2021.03; 86 (7): 5091-5101. ( PubMed , DOI )

  28. Nakajima H, Hazama Y, Sakata Y, Uchida K, Hosoya T, Yoshida S: Diverse diaryl sulfide synthesis through consecutive aryne reactions. Chem Commun. 2021.03; 57 (21): 2621-2624. ( PubMed , DOI )

  29. Matsuzawa T, Hosoya T, Yoshida S: Transition-Metal-Free Synthesis of #IN#IR-Arylphenothiazines through an #IN#IR- and #IS#IR-Arylation Sequence. Org Lett. 2021.03; 23 (6): 2347-2352. ( PubMed , DOI )

  30. Minoshima M, Uchida K, Nakamura Y, Hosoya T, Yoshida S: Acylalkylation of Arynes Generated from #Io#IR-Iodoaryl Triflates with Hydrosilanes and Cesium Fluoride. Org Lett. 2021.03; 23 (5): 1868-1873. ( PubMed , DOI )

  31. Takuya Kobayakawa, Masaru Yokoyama, Kohei Tsuji, Masayuki Fujino, Masaki Kurakami, Sayaka Boku, Miyuki Nakayama, Moemi Kaneko, Nami Ohashi, Osamu Kotani, Tsutomu Murakami, Hironori Sato & Hirokazu Tamamura: Small-Molecule Anti-HIV-1 Agents Based on HIV-1 Capsid Proteins. Biomolecules. 2021.02; 11 (2): 208. ( PubMed , DOI )

  32. Kato Daiki, Shiraishi Takuya, Kagechika Hiroyuki, Hirano Tomoya: 6-Arylcoumarin as a Scaffold of Photofunctional Molecules with OFF-ON-OFF Type Regulation JOURNAL OF ORGANIC CHEMISTRY. 2021.02; 86 (3): 2264-2270. ( PubMed , DOI )

  33. Cione, E.; Caroleo, M. C.; Kagechika, H.; Manetti, F.: Pharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands. J. Enzyme Inhibit. Med. Chem. 2021.02; 36 (1): 377-383. ( PubMed , DOI )

  34. Design, Synthesis, and Biological Evaluation of Lysine Demethylase 5 C Degraders 2021.02; 16 (10): 1609-1618. ( PubMed , DOI )

  35. Toyomoto M, Inoue A, Iida K, Denawa M, Kii I, Kadj F M N, Kishi T, Im D, Shimamura T, Onogi H, Yoshida S, Iwata S, Aoki J, Hosoya T, Hagiwara M: S1PR3–G#D12#DR-biased agonist ALESIA targets cancer metabolism and promotes glucose starvation. Cell Chem Biol. 2021.02; 28 (8): 1132-1144. ( PubMed , DOI )

  36. Takuya Kobayakawa, Kohei Tsuji, Kiju Konno, Ai Himeno, Ami Masuda, Tingting Yang, Kohei Takahashi, Yusuke Ishida, Nami Ohashi, Takeo Kuwata, Kaho Matsumoto, Kazuhisa Yoshimura, Hiromi Sakawaki, Tomoyuki Miura, Shigeyoshi Harada, Shuzo Matsushita & Hirokazu Tamamura: Hybrids of Small-Molecule CD4 Mimics with Polyethylene Glycol Units as HIV Entry Inhibitors. Journal of Medicinal Chemistry. 2021.01; 64 (3): 1481-1496. ( PubMed , DOI )

  37. Isoda M, Uetake Y, Takimoto T, Tsuda J, Hosoya T, Niwa T: Convergent Synthesis of Fluoroalkenes Using a Dual-Reactive Unit. J Org Chem. 2021.01; 86 (2): 1622-1632. ( PubMed , DOI )

  38. Yoshida S, Sakata Y, Misawa Y, Morita T, Kuribara T, Ito H, Koike Y, Kii I, Hosoya T: Assembly of four modules onto a tetraazide platform by consecutive 1,2,3-triazole formations. Chem Commun. 2021.01; 57 (7): 899-902. ( PubMed , DOI )

  39. Nishiyama Y, Akiyama K, Sakata Y, Hosoya T, Yoshida S: Facile Synthesis of Tetraarylpyrazines by Sequential Cross-coupling Approach. Chem Lett. 2021.01; 50 (1): 180-183. ( DOI )

  40. Kohei Tsuji, Rongyi Wang, Takuya Kobayakawa, Kofi Baffour-Awuah Owusu, Masayuki Fujino, Moemi Kaneko, Naoki Yamamoto, Tsutomu Murakami, Hirokazu Tamamura: Potent leads based on CA-19L, an anti-HIV active HIV-1 capsid fragment. Bioorganic & Medicinal Chemistry. 2021.01; 30 115923. ( PubMed , DOI )

  41. Fujii, S.; Sekine, R.; Kano, A.; Masuno, H.; Kawachi, E.; Hirano, T.; Kagechika, H.: Synthesis and Structure-Activity Relationship Study of 1,12-Dicarba-closo-dodecaborane-based Triol Derivatives as Nonsecosteroidal Vitamin D Analogs Heterocycles. 2021; 103 (1): 444-458. ( DOI )

  42. Arimura, M.; Tanaka, K.; Kanda, M.; Urushibara, K.; Fujii, S.*; Katagiri, K.; Azumaya, I.; Kagechika, H.; Tanatani, A.: Construction of Aromatic Multilayered Structures Based on the Conformational Properties of N,N’-Dimethylated Squaramide ChemPlusChem. 2021; 86 (1): 198-205. ( PubMed , DOI )

  43. Kouki Matsuda, Takuya Kobayakawa, Ryusho Kariya, Kiyoto Tsuchiya, Kohei Tsuji, Takahiro Ishii, Hiroyuki Gatanaga, Kazuhisa Yoshimura, Seiji Okada, Hiroaki Mitsuya, Hirokazu Tamamura & Kenji Maeda: A Therapeutic Strategy to Combat HIV-1 Latently Infected Cells With a Combination of Latency-Reversing Agents Containing DAG-Lactone PKC Activators. Frontiers in Microbiology. 2021; 12 636276. ( PubMed , DOI )

  44. Takuya Kobayakawa, Hirokazu Tamamura: Chloroalkene dipeptide isosteres as peptidomimetics. Methods in enzymology. 2021; 656 191-239. ( PubMed , DOI )

  45. Inouye S, Sumida Y, Tomabechi Y, Taguchi J, Shirouzu M, Hosoya T: Chiral deaza-coelenterazine analogs for probing a substrate-binding site in the Ca2+-binding photoprotein aequorin. PloS one. 2021; 16 (6): e0251743. ( PubMed , DOI )

  1. Sasaki H, Masuno H, Kawasaki H, Yoshihara A, Numoto N, Ito N, Ishida H, Yamamoto K, Hirata N, Kanda Y, Kawachi E, Kagechika H, Tanatani A: Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists. Journal of medicinal chemistry. 2020.12; 64 (1): 516-526. ( PubMed , DOI )

  2. Takemura H, Goto S, Hosoya T, Yoshida S: 2-Azidoacrylamides as compact platforms for efficient modular synthesis. Chem Commun (Camb). 2020.12; 56 (99): 15541-15544. ( PubMed , DOI )

  3. Idogawa R, Kim Y, Shimomori K, Hosoya T, Yoshida S: Single C–F Transformations of #Io#IR-Hydrosilyl Benzotrifluorides with Trityl Compounds as All-in-One Reagents. Org Lett. 2020.12; 22 (23): 9292-9297. ( PubMed , DOI )

  4. Takuya Kobayakawa, Kento Ebihara, Kohei Tsuji, Takuma Kawada, Masayuki Fujino, Yuzuna Honda, Nami Ohashi, Tsutomu Murakami, Hirokazu Tamamura: Bivalent HIV-1 fusion inhibitors based on peptidomimetics. Bioorg. Med. Chem. 2020.12; 28 (24): 115812. ( PubMed , DOI )

  5. Terashima N, Sakata Y, Meguro T, Hosoya T, Yoshida S: Triazole formation of phosphinyl alkynes with azides through transient protection of phosphine by copper. Chem Commun (Camb). 2020.11; 56 (90): 14003-14006. ( PubMed , DOI )

  6. Nakano-Kobayashi A, Fukumoto A, Morizane A, Nguyen D T , Le T M, Hashida K, Hosoya T, Takahashi R, Takahashi J, Hori O, Hagiwara M: Therapeutics potentiating microglial p21-Nrf2 axis can rescue neurodegeneration caused by neuroinflammation. Sci Adv. 2020.11; 6 (46): eabc1428. ( PubMed , DOI )

  7. Matsuzawa T, Hosoya T, Yoshida S: One-step synthesis of benzo[#Ib#IR]thiophenes by aryne reaction with alkynyl sulfides. Chem Sci. 2020.11; 11 (35): 9691-9696. ( DOI )

  8. Jonasson M, Nordeman P, Eriksson J, Wilking H, Wikström J, Takahashi K, Niwa T, Hosoya T, Watanabe Y, Antoni G, Sundström Poromaa I, Lubberink M, Comasco E: Quantification of aromatase binding in the female human brain using [#U11#URC]cetrozole positron emission tomography. J Neurosci Res. 2020.11; 98 (11): 2208-2218. ( PubMed , DOI )

  9. Stephen E. Miller, Kohei Tsuji, Rachel P.M. Abrams, Terrence R. Burke, Jr., Joel P. Schneider: Uncoupling the Folding-Function Paradigm of Lytic Peptides to Deliver Impermeable Inhibitors of Intracellular Protein-Protein Interactions. J. Am. Chem. Soc. 2020.11; 142 (47): 19950-19955. ( PubMed , DOI )

  10. Sato Atsushi, Shimizu Masahiro, Goto Toshiyasu, Masuno Hiroyuki, Kagechika Hiroyuki, Tanaka Nobuyuki, Shibuya Hiroshi: WNK regulates Wnt signalling and beta-Catenin levels by interfering with the interaction between beta-Catenin and GID COMMUNICATIONS BIOLOGY. 2020.11; 3 (1): ( DOI )

  11. Sakakitani S, Podyma-Inoue KA, Takayama R, Takahashi K, Ishigami-Yuasa M, Kagechika H, Harada H, Watabe T: Activation of β2-adrenergic receptor signals suppresses mesenchymal phenotypes of oral squamous cell carcinoma cells. Cancer Science. 2020.10; ( PubMed , DOI )

  12. Nakamura Y, Sakata Y, Hosoya T, Yoshida S: Synthesis of Functionalized Benzopyran/Coumarin-Derived Aryne Precursors and Their Applications. Org Lett. 2020.10; 22 (21): 8505-8510. ( PubMed , DOI )

  13. Daisuke Matsumoto, Hirokazu Tamamura, Wataru Nomura: A cell cycle-dependent CRISPR-Cas9 activation system based on an anti-CRISPR protein shows improved genome editing accuracy Communications Biology. 2020.10; 3 1-10. ( PubMed , DOI )

  14. Makio N, Sakata Y, Kuribara T, Adachi K, Hatakeyama Y, Meguro T, Igawa K, Tomooka K, Hosoya T, Yoshida S: (Hexafluoroacetylacetonato)copper(I)-cycloalkyne complexes as protected cycloalkynes. Chem Commun (Camb). 2020.09; 56 (77): 11449-11452. ( PubMed , DOI )

  15. Sato Y, Miyamoto Y, Sumida Y, Hosoya T, Ohmiya H: Boracene-based alkylborate enabled Ni/Ir hybrid catalysis. Org Biomol Chem. 2020.09; 18 (34): 6598-6601. ( PubMed , DOI )

  16. Ikeda M, Matsuzawa T, Morita T, Hosoya T, Yoshida S: Synthesis of Diverse Aromatic Ketones through C-F Cleavage of Trifluoromethyl Group. Chem Eur J. 2020.09; 26 (54): 12333-12337. ( PubMed , DOI )

  17. Kohei Tsuji, David Hymel, Terrence R. Burke, Jr.: A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors. Anal. Methods: advancing methods and applications. 2020.09; 12 (36): 4418-4421. ( PubMed , DOI )

  18. Fujii Shinya, Kikuchi Eriko, Watanabe Yuko, Suzuyama Honoka, Ishigami-Yuasa Mari, Mori Takayasu, Isobe Kiyoshi, Uchida Shinichi, Kagechika Hiroyuki: Structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 2020.09; 30 (17): 127408. ( PubMed , DOI )

  19. Sumida Y, Harada R, Sumida T, Johmoto K, Uekusa H, Hosoya T: Synthesis of Dibenzofurans by Cu-Catalyzed Deborylative Ring Contraction of Dibenzoxaborins. Org Lett. 2020.08; 22 (16): 6687-6691. ( PubMed , DOI )

  20. Adachi K, Meguro T, Sakata Y, Igawa K, Tomooka K, Hosoya T, Yoshida S: Selective strain-promoted azide-alkyne cycloadditions through transient protection of bicyclo[6.1.0]nonynes with silver or gold. Chem Commun (Camb). 2020.08; 56 (68): 9823-9826. ( PubMed , DOI )

  21. Junpeng Qi, Kohei Tsuji, David Hymel, Terrence R. Burke, Jr., Michael Hudecek, Christoph Rader, Haiyong Peng: Chemically Programmable and Switchable CAR-T Therapy Angew. Chem., Int. Ed. 2020.07; 59 (29): 12178-12185 . ( PubMed , DOI )

  22. Watanabe K, Terao N, Isao Kii, Nakagawa R, Niwa T, Hosoya T: Indolizines Enabling Rapid Uncaging of Alcohols and Carboxylic Acids by Red Light-Induced Photooxidation. Org Lett. 2020.07; 22 (14): 5434-5438. ( PubMed , DOI )

  23. Tamura Y, Minami Y, Nishiyama Y, Sakata Y, Karaki F, Hosoya T, Yoshida S: Synthesis of multisubstituted cycloalkenes through carbomagnesiation of strained cycloalkynes. Chem Commun (Camb). 2020.07; 56 (52): 7147-7150. ( PubMed , DOI )

  24. Kobayashi A, Matsuzawa T, Hosoya T, Yoshida S: One-pot Synthesis of Allyl Sulfides from Sulfinate Esters and Allylsilanes through Reduction of Alkoxysulfonium Intermediates. Chem Lett. 2020.07; 49 (7): 813-816. ( DOI )

  25. Kobayashi T, Hosoya T, Yoshida S: Aryne Reaction and Cross-Coupling Approach for the Synthesis of Diverse #IN#IR-Arylphenylalanine Derivatives. Chem Lett. 2020.07; 49 (7): 809-812. ( DOI )

  26. Inouye S, Nakamura M, Taguchi J, Hosoya T: Identification of a novel oxidation product from yellow fluorophore in the complex of apoPholasin and dehydrocoelenterazine. Bioorganic & medicinal chemistry letters. 2020.07; 30 (19): 127435. ( PubMed , DOI )

  27. Kohei Tsuji, Kofi Baffour-Awuah Owusu, Takuya Kobayakawa, Rongyi Wang, Masayuki Fujino, Moemi Kaneko, Naoki Yamamoto, Tsutomu Murakami, Hirokazu Tamamura: Exploratory studies on CA-15L, an anti-HIV active HIV-1 capsid fragment. Bioorg. Med. Chem. 2020.06; 28 (11): 115488. ( PubMed , DOI )

  28. Nakaoka T, Uetake Y, Kaneko K, Niwa T, Ochia Hi, Irie S, Suezaki Y, Otsuka N, Hayashinaka E, Wada Y, Cui Y, Maeda K, Kusuhara H, Sugiyama Y, Hosoya T, Watanabe Y: Practical synthesis of [#U18#URF]Pitavastatin and Evaluation of Hepatobiliary Transport Activity in Rats by Positron Emission Tomography. Mol Pharm. 2020.06; 17 (6): 1884-1898. ( PubMed , DOI )

  29. Wu D, Taguchi J, Tanriver M, Bode JW: Synthesis of Acylboron Compounds. Angewandte Chemie (International ed. in English). 2020.06; ( PubMed , DOI )

  30. Sato Y, Nakamura K, Sumida Y, Hashizume D, Hosoya T, Ohmiya H: Generation of Alkyl Radical through Direct Excitation of Boracene-Based Alkylborate. J Am Chem Soc. 2020.05; 142 (22): 9938-9943. ( PubMed , DOI )

  31. Nishiyama Y, Hosoya T, Yoshida S: Synthesis of benzyl sulfides via substitution reaction at the sulfur of phosphinic acid thioesters. Chem Commun (Camb). 2020.05; 56 (43): 5771-5774. ( PubMed , DOI )

  32. Kobayashi A, Matsuzawa T, Hosoya T, Yoshida S: Sulfoxide synthesis from sulfinate esters under Pummerer-like conditions. Chem Commun (Camb). 2020.05; 56 (40): 5429-5432. ( PubMed , DOI )

  33. Mutsuura K, Sakata Y, Uchida K, Hosoya T, Yoshida S: Synthesis of Thioxanthones through Formal C–H Thiolation of Benzoic Acid Esters and Acid-mediated Direct Cyclization. Chem Lett. 2020.05; 49 (7): 753-756. ( DOI )

  34. Kim Y, Kanemoto K, Shimomori K, Hosoya T, Yoshida S: Functionalization of a Single C-F Bond of Trifluoromethylarenes Assisted by an #Iortho#IR-Silyl Group Using a Trityl-Based All-in-One Reagent with Ytterbium Triflate Catalyst. Chem Eur J. 2020.05; 26 (28): 6136-6140. ( PubMed , DOI )

  35. Inouye S, Miura-Sahara Y, Iimori R, Sakata Y, Hazama Y, Yoshida S, Nakamura M, Hosoya T: A novel yellow fluorescent protein of recombinant apoPholasin with dehydrocoelenterazine. Biochem Biophys Res Commun. 2020.05; 526 (2): 404-409. ( PubMed , DOI )

  36. Kanemoto K, Sakata Y, Hosoya T, Yoshida S: Synthesis of Phenoxathiins and Phenothiazines by Aryne Reactions with Thiosulfonates. Chem Lett. 2020.05; 49 (5): 593-596. ( DOI )

  37. Takuya Kobayakawa, Hikaru Takano, Takahiro Ishii, Kohei Tsuji, Nami Ohashi, Wataru Nomura, Toshiaki Furuta, Hirokazu Tamamura: Synthesis of hydrophilic caged DAG-lactones for chemical biology applications. Org. Biomol. Chem. 2020.05; 18 (22): 4217-4223 . ( PubMed , DOI )

  38. Meguro T, Sakata Y, Morita T, Hosoya T, Yoshida S: Facile assembly of three cycloalkyne-modules onto a platform compound bearing thiophene #IS#IR,#IS#IR-dioxide moiety and two azido groups. Chem Commun (Camb). 2020.04; 56 (34): 4720-4723. ( PubMed , DOI )

  39. Erika Ishihara, Yuya Nagaoka, Toshiaki Okuno, Satoshi Kofuji, Mari Ishigami-Yuasa, Hiroyuki Kagechika, Kenya Kamimura, Shuji Terai, Takehiko Yokomizo, Yukihiko Sugimoto, Yasuyuki Fujita, Akira Suzuki, Hiroshi Nishina: Prostaglandin E2 and its receptor EP2 trigger signaling that contributes to YAP-mediated cell competition. Genes Cells. 2020.03; 25 (3): 197-214. ( PubMed , DOI )

  40. Inouye S, Sahara-Miura Y, Nakamura M, Hosoya T: Expression, purification, and characterization of recombinant apoPholasin. Protein Expr Purif. 2020.02; 171 105615. ( PubMed , DOI )

  41. Kobayashi T, Hosoya T, Yoshida S: Consecutive Aryne Generation Strategy for the Synthesis of 1,3-Diarylpyrazoles. J Org Chem. 2020.02; 85 (6): 4448-4462. ( PubMed , DOI )

  42. Niwa T, Hosoya T: Molecular Renovation Strategy for Expeditious Synthesis of Molecular Probes. Bull Chem Soc Jpn. 2020.02; 93 (2): 230-248. ( DOI )

  43. Taguchi Jumpei, Matsuura Satsuki, Seki Tomohiro, Ito Hajime: Synthesis and Tunable Optical Properties of C,N-Chelated Borate Luminophores Derived from Potassium Acyltrifluoroborates CHEMISTRY-A EUROPEAN JOURNAL. 2020.02; 26 (11): 2450-2455. ( PubMed , DOI )

  44. Itoh Yukihiro: 戦略的化学的アプローチに基づいたリシン修飾酵素のモジュレーターに関する創薬研究(Drug Discovery Researches on Modulators of Lysine-Modifying Enzymes Based on Strategic Chemistry Approaches) Chemical & Pharmaceutical Bulletin. 2020.01; 68 (1): 34-45. ( ichushi )

  45. Daisuke Matsumoto, Hirokazu Tamamura, Wataru Nomura: TALEN-Based Chemically Inducible, Dimerization-Dependent, Sequence-Specific Nucleases Biochemistry . 2020.01; 59 (2): 197-204. ( PubMed , DOI )

  46. Yazaki J, Kawashima Y, Ogawa T, Kobayashi A, Okoshi M, Watanabe T, Yoshida S, Kii I, Egami S, Amagai M, Hosoya T, Shiroguch Ki, Ohara O: HaloTag-based conjugation of proteins to barcoding-oligonucleotides. Nucleic Acids Res. 2020.01; 48 (2): e8. ( PubMed , DOI )

  47. Yeong KY, Khaw KY, Takahashi Y, Itoh Y, Murugaiyah V, Suzuki T: Discovery of gamma-mangostin from Garcinia mangostana as a potent and selective natural SIRT2 inhibitor. Bioorganic chemistry. 2020.01; 94 103403. ( PubMed , DOI )

  48. Manami Kodaka, Fengju Mao, Kyoko Arimoto-Matsuzaki, Masami Kitamura, Xiaoyin Xu, Zeyu Yang, Kentaro Nakagawa, Junichi Maruyama, Kana Ishii, Chihiro Akazawa, Takuya Oyaizu, Naoki Yamamoto, Mari Ishigami-Yuasa, Nozomi Tsuemoto, Shigeru Ito, Hiroyuki Kagechika, Hiroshi Nishina, Yutaka Hata: Characterization of a novel compound that promotes myogenesis via Akt and transcriptional co-activator with PDZ-binding motif (TAZ) in mouse C2C12 cells. PLoS ONE. 2020; 15 (4): e0231265. ( PubMed , DOI )

  49. Koga, H.; Negishi, M.; Kinoshita, M.; Fujii, S.; Mori, S.; Ishigami-Yuasa, M.; Kawachi, E.; Kagechika, H.; Tanatani, A.: Development of Androgen-Antagonistic Coumarinamides with a Unique Aromatic Folded Pharmacophore Int. J. Mol. Sci.. 2020; 21 (15): 5584. ( PubMed , DOI )

  50. Urushibara, K.; Yamada, T.; Yokoyama, A.; Mori, H.; Masu, H.; Azumaya, I.; Kagechika, H.; Yokozawa, T.; Tanatani, A.: Development of Helical Aromatic Amide Foldamers with a Diphenylacetylene Backbone J. Org. Chem.. 2020; 85 (4): 2019-2039. ( PubMed , DOI )

  51. Drug discovery researches on modulators of lysine-modifying enzymes based on strategic chemistry approaches 2020; 68 (1): 34-45. ( PubMed , DOI )

  52. Metabolic-Pathway-Oriented Screening Targeting S-Adenosyl- l -methionine Reveals the Epigenetic Remodeling Activities of Naturally Occurring Catechols 2020; 142 (1): 21-26. ( PubMed , DOI )

  1. Itoh Y, Nakashima Y, Tsukamoto S, Kurohara T, Suzuki M, Sakae Y, Oda M, Okamoto Y, Suzuki T: N+-C-H···O Hydrogen bonds in protein-ligand complexes. Scientific reports. 2019.12; 9 (1): 767. ( PubMed , DOI )

  2. Nakamura Y, Yoshida S, Hosoya T: Recent Advances in Synthetic Hetaryne Chemistry. Heterocycles. 2019.12; 98 (12): 1623-1677. ( DOI )

  3. Kitakaze K, Taniuchi S, Kawano E, Hamada Y, Miyake M, Oyadomari M, Kojima H, Kosako H, Kuribara T, Yoshida S, Hosoya T, Oyadomari S: Cell-based HTS identifies a chemical chaperone for preventing ER protein aggregation and proteotoxicity. eLife. 2019.12; 8 e43302. ( PubMed , DOI )

  4. Uchida K, Minami Y, Yoshida S, Hosoya T: Synthesis of Diverse γ-Aryl-β-ketoesters via Aryne Intermediates Generated by C-C Bond Cleavage. Org Lett. 2019.11; 21 (22): 9019-9023. ( PubMed , DOI )

  5. Nakamura Y, Ozawa S, Yoshida S, Hosoya T: Facile Synthesis of Diverse 2,6-Disubstituted Arylsilanes via Silylamination and Silylsulfanylation of Aryne Intermediates Generated from #Io#IR-Iodoaryl Triflates. Chem Lett. 2019.11; 48 (11): 1296-1299. ( DOI )

  6. Park SW, Nhieu J, Persaud SD, Miller MC, Xia Y, Lin YW, Lin YL, Kagechika H, Mayo KH, Wei LN: Publisher Correction: A new regulatory mechanism for Raf kinase activation, retinoic acid-bound Crabp1. Scientific reports. 2019.11; 9 (1): 17042. ( PubMed , DOI )

  7. Maeda Kenji, Matsuda Kouki, Islam Saiful, Kobayakawa Takuya, Tsuchiya Kiyoto, Hattori Shin-ichiro, Gatanaga Hiroyuki, Oka Shinichi, Yoshimura Kazuhisa, Tamamura Hirokazu, Mitsuya Hiroaki, Satou Yorifumi: HIV持続潜伏感染に関する最先端研究(Treatment of HIV-1-reservoirs using latency-reversing agents(LRAs) toward HIV cure) 日本エイズ学会誌. 2019.11; 21 (4): 314. ( ichushi )

  8. Hwang D, Tsuji K, Park H, Burke TR Jr, Rader C: Site-Specific Lysine Arylation as an Alternative Bioconjugation Strategy for Chemically Programmed Antibodies and Antibody-Drug Conjugates. Bioconjugate chemistry. 2019.11; 30 (11): 2889-2896. ( PubMed , DOI )

  9. Yoshida S, Goto S, Nishiyama Y, Hazama Y, Kondo M, Matsushita T, Hosoya T: Effect of Resonance on the Clickability of Alkenyl Azides in the Strain-promoted Cycloaddition with Dibenzo-fused Cyclooctynes. Chem Lett. 2019.09; 48 (9): 1038-1041. ( DOI )

  10. Mohammad Mamun Alam, Takeo Kuwata, Kazuki Tanaka, Muntasir Alam, Shokichi Takahama, Kazuya Shimura, Masao Matsuoka, Natsuki Fukuda, Hiroshi Morioka, Hirokazu Tamamura, Shuzo Matsushita: Synergistic Inhibition of Cell-to-cell HIV-1 Infection by Combinations of Single Chain Variable Fragments and Fusion Inhibitors Biochem Biophys Rep.. 2019.09; 20 100687.

  11. Masuno Hiroyuki, Kazui Yuko, Tanatani Aya, Fujii Shinya, Kawachi Emiko, Ikura Teikichi, Ito Nobutoshi, Yamamoto Keiko, Kagechika Hiroyuki: Development of novel lithocholic acid derivatives as vitamin D receptor agonists BIOORGANIC & MEDICINAL CHEMISTRY. 2019.08; 27 (16): 3674-3681. ( PubMed , DOI )

  12. Takeuchi Takumi, Taguchi Jumpei, Takahashi Rina, Masero Fabio, Ito Hajime: Concise synthesis of potassium acyltrifluoroborartes from aldehydes by borylation and oxidation ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2019.08; 258

  13. Takuya Kobayakawa, Kento Ebihara, Yuzuna Honda, Masayuki Fujino, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami, Hirokazu Tamamura: Dimeric C34 Derivatives Linked through Disulfide Bridges as New HIV-1 Fusion Inhibitors. Chembiochem. 2019.08; 20 (16): 2101-2108. ( PubMed , DOI )

  14. Uetake Y, Isoda M, Niwa T, Hosoya T: Synthesis of (2,2-Diborylvinyl)arenes by Rhodium-Catalyzed Desulfanylative #Igem#IR-Diborylation of 2-Arylvinyl Sulfides. Org Lett. 2019.07; 21 (13): 4933-4938. ( PubMed , DOI )

  15. Nakamura Y, Miyata Y, Uchida K, Yoshida S, Hosoya T: 3-Thioaryne Intermediates for the Synthesis of Diverse Thioarenes. Org Lett. 2019.07; 21 (13): 5252-5258. ( PubMed , DOI )

  16. Yoshida S, Hazama Y, Kanemoto K, Nakamura Y, Hosoya T: Facile Synthesis of Diverse #Io#IR-Iodoaryl Triflates from #Io#IR-Silylaryl Triflates by Aluminum-mediated Desilyliodination. Chem Lett. 2019.07; 48 (7): 742-745. ( DOI )

  17. Kenji Maeda, Debananda Das, Takuya Kobayakawa, Hirokazu Tamamura, Hiroaki Takeuchi: Discovery and Development of anti-HIV Therapeutic Agents: Progress Towards Improved HIV Medication. Current topics in medicinal chemistry. 2019.07; 19 (18): 1621-1649. ( PubMed , DOI )

  18. Yoshida S, Hosoya T: Target Identification of Bioactive Compounds by Photoaffinity Labeling Using Diazido Probes. Cutting-Edge Organic Synthesis and Chemical Biology of Bioactive Molecules – The Shape of Organic Synthesis to Come. 2019.06; 335-355. ( DOI )

  19. Meguro T, Chen S, Kanemoto K, Yoshida S, Hosoya T: Modular Synthesis of Unsymmetrical Doubly-ring-fused Benzene Derivatives Based on a Sequential Ring Construction Strategy Using Oxadiazinones as a Platform Molecule. Chem Lett. 2019.06; 48 (6): 582-585. ( DOI )

  20. Nishiyama Y, Misawa Y, Hazama Y, Oya K, Yoshida S, Hosoya T: Synthesis of Diverse 3-Azido-5-(azidomethyl)benzene Derivatives via Formal C–H Azidation and Functional Group-Selective Transformations. Heterocycles. 2019.06; 99 (2): 1053-1072. ( DOI )

  21. Watanabe K, Tsuda J, Ochiai H, Niwa T, Hosoya T: Divergent Synthesis of Photoaffinity Probe Candidates by Click Reactions of Azido-Substituted Aryltrifluoromethyldiazirines. Heterocycles. 2019.06; 99 (2): 1366-1387. ( DOI )

  22. Mellini P, Itoh Y, Elboray EE, Tsumoto H, Li Y, Suzuki M, Takahashi Y, Tojo T, Kurohara T, Miyake Y, Miura Y, Kitao Y, Kotoku M, Iida T, Suzuki T: Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the "Selectivity Pocket", Substrate-Binding Site, and NAD+-Binding Site. Journal of medicinal chemistry. 2019.06; 62 (12): 5844-5862. ( PubMed , DOI )

  23. Kawahara Haruka, Miyashita Naoki, Tachibana Koki, Tsuda Yusuke, Morimoto Kyohei, Tsuji Kohei, Shigenaga Akira, Otaka Akira, Ishida Tatsuhiro, Okuhira Keiichiro: A Photo-Activatable Peptide Mimicking Functions of Apolipoprotein A-I BIOLOGICAL & PHARMACEUTICAL BULLETIN. 2019.06; 42 (6): 1019-1024.

  24. Maxwell M Sakyiamah, Wataru Nomura, Takuya Kobayakawa, Hirokazu Tamamura: Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands. Bioconjug. Chem.. 2019.05; 30 (5): 1442-1450. ( PubMed , DOI )

  25. Taguchi Jumpei, Takeuchi Takumi, Takahashi Rina, Masero Fabio, Ito Hajime: Concise Synthesis of Potassium Acyltrifluoroborates from Aldehydes through Copper(I)-Catalyzed Borylation/Oxidation ANGEWANDTE CHEMIE-INTERNATIONAL EDITION. 2019.05; 58 (22): 7299-7303. ( PubMed , DOI )

  26. Jaikhan P, Buranrat B, Itoh Y, Chotitumnavee J, Kurohara T, Suzuki T: Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors. Bioorganic & medicinal chemistry letters. 2019.05; 29 (10): 1173-1176. ( PubMed , DOI )

  27. Kanemoto K, Yoshida S, Hosoya T: Synthesis of Alkynyl Sulfides by Copper-Catalyzed Thiolation of Terminal Alkynes Using Thiosulfonates. Org Lett. 2019.04; 21 (9): 3172-3177. ( PubMed , DOI )

  28. Zhao XZ, Tsuji K, Hymel D, Burke TR Jr: Development of Highly Selective 1,2,3-Triazole-containing Peptidic Polo-like Kinase 1 Polo-box Domain-binding Inhibitors. Molecules (Basel, Switzerland). 2019.04; 24 (8): 1488. ( PubMed , DOI )

  29. Ota Yosuke, Nakamura Arisa, Elboray Elghareeb E., Itoh Yukihiro, Suzuki Takayoshi: 創薬　近年の進歩と将来　5-フルオロウラシルとLSD1阻害薬の複合体のデザイン、合成および生物学的評価(Drug Discovery: Recent Progress and the Future: Design, Synthesis, and Biological Evaluation of a Conjugate of 5-Fluorouracil and an LSD1 Inhibitor) Chemical & Pharmaceutical Bulletin. 2019.03; 67 (3): 192-195. ( ichushi )

  30. Takuya Kobayakawa, Kiju Konno, Nami Ohashi, Kohei Takahashi, Ami Masuda, Kazuhisa Yoshimura, Shigeyoshi Harada, Hirokazu Tamamura: Soluble-type small-molecule CD4 mimics as HIV entry inhibitors BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 2019.03; 29 (5): 719-723. ( PubMed , DOI )

  31. Ishigami-Yuasa, M.; Ekimoto, H.; Kagechika, H.: Class IIb HDAC inhibition enhances the inhibitory effect of Am80, a synthetic retinoid, in prostate cancer Biol. Pharm. Bull.. 2019.03; 42 (3): 448-452. ( PubMed , DOI )

  32. Hogan M, Bahta M, Tsuji K, Nguyen TX, Cherry S, Lountos GT, Tropea JE, Zhao BM, Zhao XZ, Waugh DS, Burke TR Jr, Ulrich RG: Targeting Protein-Protein Interactions of Tyrosine Phosphatases with Microarrayed Fragment Libraries Displayed on Phosphopeptide Substrate Scaffolds. ACS combinatorial science. 2019.03; 21 (3): 158-170. ( PubMed , DOI )

  33. Yoshida S, Kuribara T, Ito H, Meguro T, Nishiyama Y, Karaki F, Hatakeyama Y, Koike Y, Kii I, Hosoya T: A facile preparation of functional cycloalkynes via an azide-to-cycloalkyne switching approach. Chem Commun. 2019.03; 55 (24): 3556-3559. ( PubMed , DOI )

  34. Maxwell M. Sakyiamah, Takuya Kobayakawa, Masayuki Fujino, Makoto Konno, Tetsuo Narumi, Tomohiro Tanaka, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami, Hirokazu Tamamura: Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands BIOORGANIC & MEDICINAL CHEMISTRY. 2019.03; 27 (6): 1130-1138. ( PubMed , DOI )

  35. Miyake Y, Itoh Y, Hatanaka A, Suzuma Y, Suzuki M, Kodama H, Arai Y, Suzuki T: Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy. Bioorganic & medicinal chemistry. 2019.03; 27 (6): 1119-1129. ( PubMed , DOI )

  36. Akinobu Z. Suzuki, Ryota Sekine, Shiori Takeda, Ryosuke Aikawa, Yukiko Shiraishi, Tomomi Hamaguchi, Hiroyuki Okuno, Tamamura Hirokazu, Furuta Toshiaki: A clickable caging group as a new platform for modular caged compounds with improved photochemical properties CHEMICAL COMMUNICATIONS. 2019.01; 55 (4): 451-454. ( PubMed , DOI )

  37. Toyoda Y, Morimoto K, Suno R, Horita S, Yamashita K Hirata K, Sekiguchi Y, Yasuda S, Shiroishi M, Shimizu T, Urushibata Y, Kajiwara Y, Inazumi T, Hotta Y, Asada H, Nakane T, Shiimura Y, Nakagita T, Tsuge K, Yoshida S, Kuribara T, Hosoya T, Sugimoto Y, Nomura N, Sato M, Hirokawa T, Kinoshita M, Murata T, Takayama K, Yamamoto M, Narumiya S, Iwata S, Kobayashi T: Ligand binding to human prostaglandin E receptor EP4 at the lipid-bilayer interface. Nat Chem Biol. 2019.01; 15 (1): 18-26. ( PubMed , DOI )

  38. Kouki Matsuda, Takuya Kobayakawa, Kiyoto Tsuchiya, Shin-Ichiro Hattori, Wataru Nomura, Hiroyuki Gatanaga, Kazuhisa Yoshimura, Shinichi Oka, Yasuyuki Endo, Hirokazu Tamamura, Hiroaki Mitsuya, Kenji Maeda: Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C-induced HIV latency reversal. J. Biol. Chem.. 2019.01; 294 (1): 116-129. ( PubMed , DOI )

  39. Yokoo, H.; Kagechika, H.; Ohsaki, A; Hirano T.: A Polarity-Sensitive Fluorescent Amino Acid and its Incorporation into Peptides for the Ratiometric Detection of Biomolecular Interactions ChemPlusChem. 2019; 84 1716-1719. ( DOI )

  40. Mori, S.; Tsuemoto, N.; Kasagawa, T.; Nakano, E.; Fujii, S.; Kagechika, H.: Development of Boron-Cluster-Based Progesterone Receptor Antagonists Bearing a Pentafluorosulfanyl (SF5) Chem. Pharm. Bull.. 2019; 67 (12): 1278-1283.

  41. Mori, S.; Iinuma, H.; Manaka, N.; Ishigami-Yuasa, M.; Murayama, T.; Nishijima, Y.; Sakurai, A.; Arai, R.; Kurebayashi, N.; Sakurai, T.; Kagechika, H.: Structural development of a type-1 ryanodine receptor (RyR1) Ca2+-release channel inhibitor guided by endoplasmic reticulum Ca2+ assay Eur. J. Med. Chem.. 2019; 179 837-848. ( PubMed , DOI )

  42. Endo, Y.; Sugiura, Y.; Funasaki, M.; Kagechika, H.; Ishibashi, M.; Ohsaki, A.: Two new alkaloids from Crinum asiaticum var. japonicum. J. Nat. Med.. 2019; 73 (3): 648-652. ( PubMed , DOI )

  43. Kaitoh, K.; Nakatsu, A.; Mori, S.; Kagechika, H.; Hashimoto, Y.; Fujii, S.: Design, synthesis and biological evaluation of novel nonsteroidal progesterone receptor antagonists based on phenylamino-1,3,5-tirazine scaffold Chem. Pharm. Bull.. 2019; 67 (6): 566-575. ( PubMed , DOI )

  44. Park, S. W.; Nhieu, J.; Persaud, S. D.; Miller, M. C.; Xia, Y.; Lin, Y.-W.; Lin, Y.-L.; Kagechika, H.; Mayo, K. H.; Wei, L.-N.: A new regulatory mechanism for Raf kinase activation, retinoic acid-bound Crabp1 Sci. Rep.. 2019; 9 10929. ( DOI )

  45. McDonald, M. G.; Yeung, C. K.; Teitelbaum, A. M.; Johnson, A. L.; Fujii, S.; Kagechika, H.; A New LC-MS Assay for the Quantitative Analysis of Vitamin K Metabolites in Human Urine Rettie, A. E.: A New LC-MS Assay for the Quantitative Analysis of Vitamin K Metabolites in Human Urine J. Lipid Res.. 2019; 60 (4): 892-899. ( DOI )

  46. Kanda, M.; Urushibara, Ko.; Park, S.; Fujii, S.; Masu, H.; Katagiri, K.; Azumaya, I.; Kagechika, H.; Tanatani, A.: Spontaneous Chiral Resolution of N,N’-Diarylsquaramides : Formation of Various Types of One-handed Helical Networks During Crystallization Tetrahedron . 2019; 75 (19): 2771-2777. ( DOI )

  47. Fujii, S.; Yanagida, N.; Mori, S.; Kawachi, E.; Kagechika, H: Design and synthesis of cyclohexyl-p-carborane derivatives as a new class of progesterone receptor antagonists Heterocycles . 2019; 99 (1): 425-445. ( DOI )

  48. Mori S, Tsuemoto N, Kasagawa T, Nakano E, Fujii S, Kagechika H: Development of Boron-Cluster-Based Progesterone Receptor Antagonists Bearing a Pentafluorosulfanyl (SF5) Group. Chemical & pharmaceutical bulletin. 2019; 67 (12): 1278-1283. ( PubMed , DOI )

  49. Ota Y, Nakamura A, Elboray EE, Itoh Y, Suzuki T: Design, Synthesis, and Biological Evaluation of a Conjugate of 5-Fluorouracil and an LSD1 Inhibitor. Chemical & pharmaceutical bulletin. 2019; 67 (3): 192-195. ( PubMed , DOI )

  1. Itoh Y: Chemical Protein Degradation Approach and its Application to Epigenetic Targets. Chemical record (New York, N.Y.). 2018.12; 18 (12): 1681-1700. ( PubMed , DOI )

  2. Urushibara, K.; Masu, H.; Mori, H.; Azumaya, I.; Hirano, T.; Kagechika,H.; Tanatani, A. : Synthesis and Conformational Analysis of Alternately N-Alkylated Aromatic Amide Oligomers J. Org. Chem.. 2018.11; 83 (23): 14338-14349. ( PubMed , DOI )

  3. Takuya Kobayakawa, Nami Ohashi, Yuki Hirota, Kohei Takahashi, Yuko Yamada, Tetsuo Narumi, Kazuhisa Yoshimura, Shuzo Matsushita, Shigeyoshi Harada, Hirokazu Tamamura: Flexibility of small molecular CD4 mimics as HIV entry inhibitors. Bioorg. Med. Chem.. 2018.11; 26 (21): 5664-5671. ( PubMed , DOI )

  4. Wataru Nomura, Daisuke Matsumoto, Taisuke Sugii, Takuya Kobayakawa, Hirokazu Tamamura: Efficient and Orthogonal Transcription Regulation by Chemically Inducible Artificial Transcription Factors. Biochemistry. 2018.11; 57 (45): 6452-6459. ( PubMed , DOI )

  5. Zhang Z, Niwa T, Watanabe Y, Hosoya T: Palladium(II)-mediated rapid #U11#URC-cyanation of (hetero)arylborons. Org Biomol Chem. 2018.11; 16 (41): 7711-7716. ( PubMed , DOI )

  6. Takahashi K, Hosoya T, Onoe K, Takashima T, Tanaka M, Ishii A, Nakatomi Y, Tazawa S, Takahashi K, Doi H, Wada Y, Watanabe Y: Association between aromatase in human brains and personality traits. Sci Rep. 2018.11; 8 (1): 16841. ( PubMed , DOI )

  7. Yoshida S, Tanaka J, Nishiyama Y, Hazama Y, Matsushita T, Hosoya T: Further enhancement of the clickability of doubly sterically-hindered aryl azides by #Ipara#IR-amino substitution. Chem Commun. 2018.11; 54 (96): 13499-13502. ( PubMed , DOI )

  8. Kazui, Y.; Fujii, S.; Yamada, A.; Ishigami-Yuasa, M.; Kagechika, H.; Tanatani, A.: Structure-Activity Relationship of Novel Androgen Receptor Antagonists Bearing a (Benzoylaminophenoxy)phenol Pharmacophore. Bioorg. Med. Chem.. 2018.10; 26 (18): 5118-5127. ( PubMed , DOI )

  9. Timalsina, S.; Arimoto-Matsuzaki, K.; Kitamura, M.; Xu, X.; Wenzhe, Q.; Ishigami-Yuasa, M.; Kagechika, H.; Hata, Y.: Chemical compounds that suppress hypoxia-induced stress granule formation enhance cancer drug sensitivity of human cervical cancer HeLa cells. J. Biochem.. 2018.10; 164 (5): 381-391. ( PubMed , DOI )

  10. Hymel D, Grant RA, Tsuji K, Yaffe MB, Burke TR Jr: Histidine N(τ)-cyclized macrocycles as a new genre of polo-like kinase 1 polo-box domain-binding inhibitors. Bioorganic & medicinal chemistry letters. 2018.10; 28 (19): 3202-3205. ( PubMed , DOI )

  11. Sumida Y, Harada R, Sumida T, Hashizume D, Hosoya T: Hydrosilyl Group-directed Iridium-catalyzed peri-Selective C–H Borylation of Ring-fused (Hetero)Arenes. Chem Lett. 2018.10; 47 (10): 1251-1254. ( DOI )

  12. Matsuzawa T, Yoshida S, Hosoya T: Recent advances in reactions between arynes and organosulfur compounds. Tetrahedron Lett. 2018.10; 59 (48): 4197-4208 . ( DOI )

  13. Itoh Y, Suzuki M: Design, synthesis, and biological evaluation of novel ubiquitin-activating enzyme inhibitors. Bioorganic & medicinal chemistry letters. 2018.09; 28 (16): 2723-2727. ( PubMed , DOI )

  14. Loppi, S.; Kolosowska, N.; Kärkkäinen, O.; Korhonen, P.; Huuskonen, M.; Grubman, A.; Dhungana, H.; Wojciechowski, S.; Pomeshchik, Y.; Giordano, M.; Kagechika, H.; White, A.; Auriola, S.; Koistinaho, J.; Landreth, G.; Hanhineva, K.; Kanninen, K.; Malm, T.: HX600, a synthetic agonist for RXR-Nurr1 heterodimer complex, preventsischemia-induced neuronal damag Brain Behav. Immunol.. 2018.09; 73 670-681. ( DOI )

  15. Li, M.; Qin, X.-Y.; Furutani, Y.; Inoue, I.; Sekihara, S.; Kagechika, H.; Kojima S.: Prevention of acute liver injury by suppressing plasma kallikrein-dependent activation of latent TGF-β Biochem. Biophys. Res. Chem.. 2018.09; 504 (4): 857-864. ( PubMed , DOI )

  16. Inouye S, Tomabechi Y, Hosoya T, Sekine S, Shirouzu M: Slow luminescence kinetics of semi-synthetic aequorin: expression, purification and structure determination of #Icf3#IR-aequorin. J Biochem. 2018.09; 164 (3): 247-255. ( PubMed , DOI )

  17. Nishiyama Y, Kamada S, Yoshida S, Hosoya T: Generation of Arynes by Selective Cleavage of a Carbon–Phosphorus Bond of #Io#IR-(Diarylphosphinyl)aryl Triflates Using a Grignard Reagent. Chem Lett. 2018.09; 47 (9): 1216-1219. ( DOI )

  18. Hirano, T.; Fujiwara, T.; Niwa, H.; Hirano, M.; Ohira, K.; Okazaki, Y.; Sato, S.; Umehara, T.; Maemoto, Y.; Ito, A.; Yoshida, M.; Kagechika, H.: Development of novel inhibitors for histone methyltransferase SET7/9 based on cyproheptadine ChemMedChem. 2018.08; 13 (15): 1530-1540. ( PubMed , DOI )

  19. Takahashi Rina, Taguchi Jumpei, Bode Jeffery, Ito Hajime: Synthesis of alpha-amino acylboron bearing hydroxylamine moiety for preparation of peptides bearing acylboron moiety ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2018.08; 256

  20. Taguchi Jumpei, Ikeda Toshiki, Takahashi Rina, Sasaki Ikuo, Bode Jeffery, Ito Hajime: Concise synthesis of acylboronates by ozonolysis and their application to oligopeptide synthesis ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2018.08; 256

  21. Fujii, S.; Mori, S.; Kagechika, H.; Parra, M. A. M.; Gronemeyer, H.: Development of biotin-retinoid conjugates as chemical probes for analysis of retinoid function. Bioorg. Med. Chem. Lett.. 2018.07; 28 (14): 2442-2445. ( PubMed , DOI )

  22. Nishiyama, Y.; Mori, S.; Makishima, M.; Fujii, S.; Kagechika, H.; Hashimoto, Y.; Ishikawa, M.: Novel non-steroidal progesterone receptor (PR) antagonists with a phenanthridinone skeleton. ACS Med. Chem. Lett.. 2018.07; 9 (7): 641-645. ( PubMed , DOI )

  23. Meguro T, Terashima N, Ito H, Koike Y, Kii I, Yoshida S, Hosoya T: Staudinger reaction using 2,6-dichlorophenyl azide derivatives for robust aza-ylide formation applicable to bioconjugation in living cells. Chem Commun. 2018.07; 54 (57): 7904-7907. ( PubMed , DOI )

  24. Matsuzawa T, Uchida K, Yoshida S, Hosoya T: Synthesis of Diverse Phenothiazines by Direct Thioamination of Arynes with #IS#IR-(#Io#IR-Bromoaryl)-#IS#IR-methylsulfilimines and Subsequent Intramolecular Buchwald–Hartwig Amination. Chem Lett. 2018.07; 47 (7): 825-828. ( DOI )

  25. Kei Toyama, Wataru Nomura, Takuya Kobayakawa, Hirokazu Tamamura: Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR. Bioconjug. Chem.. 2018.06; 29 (6): 2050-2057. ( PubMed , DOI )

  26. Qin, X.-Y.; Suzuki, H.; Honda, M.; Okada, H.; Kaneko, S.; Inoue, I.; Ebisui, E.; Hashimoto, K.; Carninci, P.; Kanki, K.; Tatsukawa, H.; Ishibashi, N.; Masaki, T.; Matsuura, T.; Kagechika, H.; Toriguchi, K.; Hatano, E.; Shirakami, Y.; Shiota, G.; Shimizu, M.; Moriwaki, H.; Kojima, S. : Prevention of hepatocellular carcinoma by targeting MYCN-positive liver cancer stem cells with acyclic retinoid. Proc. Nat. Acad. Sci. USA. 2018.06; 115 (19): 4969-4974. ( PubMed , DOI )

  27. Murayama, T.; Kurebayashi, Ishigami-Yuasa, M.; Mori, A.; Suzuki, Y.; Akima, R.; Ogawa, H.; Suzuki, J.; Kanemaru, K.; Oyamada, H.; Kiuchi, Y.; Iino, K.; Kagechika, H.; Sakurai, T. : Efficient High-Throughput Screening by Endoplasmic Reticulum Ca2+ Measurement to Identify Inhibitors of Ryanodine Receptor Ca2+-Release Channels Mol. Pharmacol. . 2018.06; 94 (1): 722-730. ( PubMed , DOI )

  28. Yoshida S, Kuribara T, Morita T, Matsuzawa T, Morimoto K, Kobayashi T, Hosoya T: Expanding the synthesizable multisubstituted benzo[#Ib#IR]thiophenes via 6,7-thienobenzynes generated from #Io#IR-silylaryl triflate-type precursors. RSC Adv. 2018.06; 8 (39): 21754-21758. ( DOI )

  29. Meguro T, Yoshida S, Igawa K, Tomooka K, Hosoya T: Transient Protection of Organic Azides from Click Reactions with Alkynes by Phosphazide Formation. Org Lett. 2018.06; 20 (13): 4126-4130. ( PubMed , DOI )

  30. Tojo, Y.; Urushibara, K.; Yamamoto, S.; Mori, H.; Masu, H.; Kudo, M.; Hirano, T.; Azumaya, I.; Kagechika, H.; Tanatani, A.: Conformational Properties of Aromatic Oligoamides Bearing Pyrrole Rings. J. Org. Chem.. 2018.04; 83 (8): 4606-4617. ( PubMed , DOI )

  31. Park, S.; Uchida, J.; Urushibara, K.; Kagechika, H.; Kato, T.; Tanatani, A.: Self-assembly of Liquid-crystalline Squaramides. Chem. Lett.. 2018.04; 47 (4): 601-604. ( DOI )

  32. Urushitani, H.; Katsu, Y.; Kagechika, H.; Sousa, A. C. A.; Barroso, C. M.; Ohta, Y.; Shiraishi, H.; Iguchi, T.; Horiguchi, T.: Characterization and comparison of transcriptional activities of the retinoid X receptors by various organotin compounds in three prosobranch gastropods; Thais clavigera, Nucella lapillus and Babylonia japonica. Aquatic Toxicol. . 2018.04; 199 103-115. ( PubMed , DOI )

  33. Wataru Nomura, Daisuke Matsumoto, Taisuke Sugii, Takuya Kobayakawa: Chemically-controlled orthogonal regulation of multiple endogenous genes FASEB Journal. 2018.04; 32 (1):

  34. Yoshida S, Kanno K, Kii I, Misawa Y, Hagiwara M, Hosoya T: Convergent synthesis of trifunctional molecules by three sequential azido-type-selective cycloadditions. Chem Commun. 2018.04; 54 (30): 3705-3708. ( PubMed , DOI )

  35. Kii I, Hirahara-Owada S, Yamaguchi M, Niwa T, Koike Y, Sonamoto R, Ito H, Takahashi K, Yokoyama C, Hayashi T, Hosoya T, Watanabe Y: Quantification of receptor activation by oxytocin and vasopressin in endocytosis-coupled bioluminescence reduction assay using nanoKAZ. Anal Biochem. 2018.04; 549 174-183. ( PubMed , DOI )

  36. Ando F, Mori S, Yui N, Morimoto T, Nomura N, Sohara E, Rai T, Sasaki S, Kondo Y, Kagechika H, Uchida S: AKAPs-PKA disruptors increase AQP2 activity independently of vasopressin in a model of nephrogenic diabetes insipidus Nat Commun. 2018.04; 9 (1): 1411. ( PubMed , DOI )

  37. Shu Shimada, Yoshimitsu Akiyama, Kaoru Mogushi, Mari Ishigami-Yuasa, Hiroyuki Kagechika, Hiromi Nagasaki, Hiroshi Fukamachi, Yasuhito Yuasa, Shinji Tanaka: Identification of selective inhibitors for diffuse-type gastric cancer cells by screening of annotated compounds in preclinical models. Br. J. Cancer. 2018.04; 118 (7): 972-984. ( PubMed , DOI )

  38. Ajiro M, Sakai H, Onogi H, Yamamoto M, Sumi E, Sawada T, Nomura T, Kabashima K, Hosoya T, Hagiwara M: CDK9 Inhibitor FIT-039 Suppresses Viral Oncogenes E6 and E7 and Has a Therapeutic Effect on HPV-Induced Neoplasia. Clin Cancer Res. 2018.04; ( PubMed , DOI )

  39. Yokoo, H.; Ohsaki, A.; Kagechika, H.; Hirano, T.: Unique properties of 1,5-naphthyridin-2(1H)-one derivatives as environmental-polarity-sensitive fluorescent dyes. Eur. J. Org. Chem.. 2018.03; 2018 (5): 679-687. ( DOI )

  40. Tsukamoto S, Sakae Y, Itoh Y, Suzuki T, Okamoto Y: Computational analysis for selectivity of histone deacetylase inhibitor by replica-exchange umbrella sampling molecular dynamics simulations. The Journal of chemical physics. 2018.03; 148 (12): 125102. ( PubMed , DOI )

  41. Junichi Maruyama, Kazutoshi Inami, Fumiyoshi Michishita, Xinliang Jiang, Hiroaki Iwasa, Kentaro Nakagawa, Mari Ishigami-Yuasa, Hiroyuki Kagechika, Norio Miyamura, Jun Hirayama, Hiroshi Nishina, Daichi Nogawa, Kouhei Yamamoto, Yutaka Hata: Novel YAP1 Activator, Identified by Transcription-Based Functional Screen, Limits Multiple Myeloma Growth. Mol. Cancer Res.. 2018.02; 16 (2): 197-211. ( PubMed , DOI )

  42. Ota Y, Miyamura S, Araki M, Itoh Y, Yasuda S, Masuda M, Taniguchi T, Sowa Y, Sakai T, Itami K, Yamaguchi J, Suzuki T: Design, synthesis and evaluation of γ-turn mimetics as LSD1-selective inhibitors. Bioorganic & medicinal chemistry. 2018.02; 26 (3): 775-785. ( PubMed , DOI )

  43. Takuya Kobayakawa, Yudai Matsuzaki, Kentaro Hozumi, Wataru Nomura, Motoyoshi Nomizu, Hirokazu Tamamura: Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application. ACS Medicinal Chemistry Letters. 2018.01; 9 (1): 6-10. ( PubMed , DOI )

  44. Kakizawa T, Ota Y, Itoh Y, Suzuki T: Histone H3 peptides incorporating modified lysine residues as lysine-specific demethylase 1 inhibitors. Bioorganic & medicinal chemistry letters. 2018.01; 28 (2): 167-169. ( PubMed , DOI )

  45. Kanemoto K, Yoshida S, Hosoya T: Modified Conditions for Copper-Catalyzed #Iipso#IR-Thiolation of Arylboronic Acid Esters with Thiosulfonates. Chem Lett. 2018.01; 47 (1): 85-88. ( DOI )

  46. Kei Toyama, Takuya Kobayakawa, Wataru Nomura, Hirokazu Tamamura: Inhibition of EGFR Activation by Bivalent Ligands Based on a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR. Chem. Pharm. Bull.. 2018; 66 (11): 1083-1089. ( PubMed , DOI )

  47. Ota Y, Kakizawa T, Itoh Y, Suzuki T: Design, Synthesis, and In Vitro Evaluation of Novel Histone H3 Peptide-Based LSD1 Inactivators Incorporating α,α-Disubstituted Amino Acids with γ-Turn-Inducing Structures. Molecules (Basel, Switzerland). 2018; 23 (5): ( PubMed , DOI )

  1. Kusuhara H, Takashima T, Fujii H, Takashima T, Tanaka M, Ishii A, Tazawa S, Takahashi K, Takahashi K, Tokai H, Yano T, Kataoka M, Inano A, Yoshida S, Hosoya T, Sugiyama Y, Yamashita S, Hojo T, Watanabe Y: Comparison of pharmacokinetics of newly discovered aromatase inhibitors by a cassette microdosing approach in healthy Japanese subjects. Drug Metab Pharmacokinet. 2017.12; 32 (6): 293-300. ( PubMed , DOI )

  2. Mori, S.; Takagaki, R.; Fujii, S.; Urushibara, K.; Tanatani, A.; Kagechika, H.: Novel non-steroidal progesterone receptor ligands based on m-carborane containing a secondary alcohol: effect of chirality on ligand activity Chem. Pharm. Bull.. 2017.11; 65 (11): 1051-1057. ( PubMed , DOI )

  3. Endo,Y.; Kasahara,T.; Harada,K.; Kubo, M.; Etoh, T.; Ishibashi, M.; Ishiyama, A.; Iwatsuki, M.; Otoguro, K.; Ohmura, S.; Akisue, G.; Hirano, T.; Kagechika, H.; Fukuyama, Y.; Ohsaki, A.: Sucupiranins A−L, Furanocassane Diterpenoids from the Seeds of Bowdichia virgilioides. J. Nat. Prod. . 2017.11; 80 (12): 3120-3127. ( PubMed , DOI )

  4. Yoshida S, Shimizu K, Uchida K, Hazama Y, Igawa K, Tomooka K, Hosoya T: Construction of Condensed Polycyclic Aromatic Frameworks through Intramolecular Cycloaddition Reactions Involving Arynes Bearing an Internal Alkyne Moiety. Chem Eur J. 2017.11; 23 (61): 15332-15335. ( PubMed , DOI )

  5. Hoang, H. N.; Granero-Fernandez, E.; Yamada, S.; Mori, S.; Kagechika, H.; Medina-Gonzalez, Y.; Matsuda, T.: Modulating Biocatalytic Activity toward Sterically Bulky Substrates in CO2-Expanded Biobased Liquids by Tuning the Physicochemical Properties. ACS Sus. Chem. Eng.. 2017.10; 5 (11): 11051-11059. ( DOI )

  6. Taguchi Jumpei, Ikeda Toshiki, Takahashi Rina, Sasaki Ikuo, Ogasawara Yasushi, Dairi Tohru, Kato Naoya, Yamamoto Yasunori, Bode Jeffrey W., Ito Hajime: Synthesis of Acylborons by Ozonolysis of Alkenylboronates: Preparation of an Enantioenriched Amino Acid Acylboronate ANGEWANDTE CHEMIE-INTERNATIONAL EDITION. 2017.10; 56 (44): 13847-13851. ( PubMed , DOI )

  7. Tanegashima Kosuke, Takahashi Rena, Nuriya Hideko, Iwase Rina, Naruse Naoto, Tsuji Kohei, Shigenaga Akira, Otaka Akira, Hara Takahiko: CXCL14 Acts as a Specific Carrier of CpG DNA into Dendritic Cells and Activates Toll-like Receptor 9-mediated Adaptive Immunity EBIOMEDICINE. 2017.10; 24 247-256. ( PubMed , DOI )

  8. Matsuzawa T, Uchida K, Yoshida S, Hosoya T: Synthesis of Diverse #Io#IR-Arylthio-Substituted Diaryl Ethers by Direct Oxythiolation of Arynes with Diaryl Sulfoxides Involving Migratory #IO#IR-Arylation. Org Lett. 2017.10; 19 (20): 5521-5524. ( PubMed , DOI )

  9. Hatakeyama M, Sakamoto Y, Ogata K, Sumida Y, Sumida T, Hosoya T, Nakamura S: A study on an unusual S#DN#DR2 mechanism in the methylation of benzyne through nickel-complexation. Phys Chem Chem Phys. 2017.10; 19 (39): 26926-26933. ( PubMed , DOI )

  10. Yamasaki, R.; Iida, M.; Ito, A.; Fukuda, K.; Tanatani, A.; Kagechika, H., Masu, H. Okamoto, I. : Crystal Engineering of N,N’-Diphenylurea Compounds Featuring Phenyl-Perfluorophenyl Interaction Crystal Growth Des.. 2017.09; 17 5858-5866.

  11. Niwa T, Ochiai H, Hosoya T: Facile Transformation of α,β-Unsaturated Carboxylic Acids to Alkenylboronic Esters via Rhodium-Catalyzed Decarbonylative Borylation of α,β-Unsaturated Thioesters. Chem Lett. 2017.09; 46 (9): 1315-1318. ( DOI )

  12. Kanemoto K, Sugimura Y, Shimizu S, Yoshida S, Hosoya T: Rhodium-catalyzed odorless synthesis of diaryl sulfides from borylarenes and #IS#IR-aryl thiosulfonates. Chem Commun. 2017.09; 53 (77): 10640-10643. ( PubMed , DOI )

  13. Sakaguchi H, Uetake Y, Ohashi M, Niwa T, Ogoshi S, Hosoya T: Copper-Catalyzed Regioselective Monodefluoroborylation of Polyfluoroalkenes en Route to Diverse Fluoroalkenes. J Am Chem Soc. 2017.09; 139 (36): 12855-12862. ( PubMed , DOI )

  14. Nakano-Kobayashi A, Awaya T, Kii I, Sumida Y, Okuno Y, Yoshida S, Sumida T, Inoue H, Hosoya T, Hagiwara M: Prenatal neurogenesis induction therapy normalizes brain structure and function in Down syndrome mice. Proc Natl Acad Sci USA. 2017.09; 114 (38): 10268-10273. ( PubMed , DOI )

  15. Suzuki, D.; Saito-Hakoda, A.; Ito, R.; Shimizu, K.; Parvin, R.; Shimada, H.; Noro, E.; Suzuki, S.; Fujiwara, I.; Kagechika, H.; Rainey, W. E.; Kure, S.; Ito, S.; Yokoyama, A.; Sugawara, A. : Suppressive effects of RXR agonist PA024 on adrenal CYP11B2 expression, aldosterone secretion and blood pressure Plos ONE. 2017.08; 12 (8): e0181055. ( PubMed , DOI )

  16. Nomura Wataru, Matsumoto Daisuke, Hashimoto Tsukasa, Sugii Taisuke, Tamamura Hirokazu: Development of chemical-inducible artificial transcription factors based on sequence-specific DNA binders ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2017.08; 254

  17. Meguro T, Yoshida S, Hosoya T: Sequential Molecular Conjugation using Thiophene #IS#IR,#IS#IR-Dioxides Bearing a Clickable Functional Group. Chem Lett. 2017.08; 46 (8): 1137-1140. ( DOI )

  18. Ohashi N, Kobayashi R, Nomura W, Kobayakawa T, Czikora A, Herold B K, Lewin N E, Blumberg P M, Tamamura H: Synthesis and Evaluation of Dimeric Derivatives of Diacylglycerol-Lactones as Protein Kinase C Ligands. Bioconjugate Chem. 2017.07; ( DOI )

  19. Takuya Kobayakawa, Hirokazu Tamamura: Stereoselective synthesis of Xaa-Yaa type (Z)-chloroalkene dipeptide isosteres via efficient utilization of organocopper reagents mediated allylic alkylation Tetrahedron. 2017.07; 73 (30): 4464-4471. ( DOI )

  20. Nishiyama Y, Hazama Y, Yoshida S, Hosoya T: Synthesis of Unsymmetrical Tertiary Phosphine Oxides via Sequential Substitution Reaction of Phosphonic Acid Dithioesters with Grignard Reagents. Org Lett. 2017.07; 19 (14): 3899-3902. ( PubMed , DOI )

  21. Mori, S.; Hirano T.; Takaguchi, A.; Fujiwara, T.; Okazaki, Y.; Kagechika, H.: Selective Reagent for Detection of N-ε-Monomethylation of a Peptide Lysine Residue through SNAr Reaction European Journal of Organic Chemistry. 2017.07; 3606-3611.

  22. Yoshioka, H.; Yamada, A.; Nishiyama, Y.; Kagechika, H.; Hashimoto, Y.; Fujii, S.: Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold Bioorganic and Medicinal Chemistry. 2017.07; 25 (13): 3461-3470.

  23. Yoshizaki, Y.; Mori, T.; Ishigami-Yuasa, M.; Kikuchi, E.; Takahashi, D.; Zeniya, M.; Nomura, N.; Mori, Y.; Araki, Y.; Ando, F.; Mandai, S.; Kasagi, Y.; Arai, Y.; Sasaki, E.; Yoshida, S.; Kagechika, H.; Rai, T.; Uchida, S.; Sohara, E.: Drug-Repositioning Screening for Keap1-Nrf2 Binding Inhibitors using Fluorescence Correlation Spectroscopy Science Reports. 2017.07; 7 3945.

  24. Kobayakawa Takuya, Tamamura Hirokazu: Stereoselective synthesis of Xaa-Yaa type (Z)-chloroalkene dipeptide isosteres via efficient utilization of organocopper reagents mediated allylic alkylation TETRAHEDRON. 2017.07; 73 (30): 4464-4471. ( DOI )

  25. Furubayashi T, Motohashi K, Wakao K, Matsuda T, Kii I, Hosoya T, Hayashi N, Sadaie M, Ishikawa F, Matsushita M, Fujiyoshi S: Three-Dimensional Localization of an Individual Fluorescent Molecule with Angstrom Precision. J Am Chem Soc. 2017.07; 139 (26): 8990-8994. ( PubMed , DOI )

  26. Nakamura Y, Yoshida S, Hosoya T: Facile Synthesis of Phthalides from Methyl #Iortho#IR-Iodobenzoates and Ketones via an Iodine–Magnesium Exchange Reaction Using a Silylmethyl Grignard Reagent. Chem Lett. 2017.06; 46 (6): 858-861. ( DOI )

  27. Sumida Y, Sumida T, Hosoya T: Nickel-Catalyzed Reductive Cross-Coupling of Aryl Triflates and Nonaflates with Alkyl Iodides. Synthesis. 2017.06; 49 (16): 3590-3601. ( DOI )

  28. Ishigami-Yuasa, M.; Watanabe, Y.; Mori, T.; Masuno, H.; Fujii, S.; Kikuchi, E.; Uchida, S.; Kagechika, H.: Development of WNK signaling inhibitors as a new class of antihypertensive drugs Bioorganic and Medicinal Chemistry. 2017.06; 25 (14): 3845-3852.

  29. Nguyen, B. N.; Okuno, Y.; Ajiro, M.; Iida, K.; Denawa, M.; Yamamoto, M.; Sakamoto, N.; Kagechika, H.; Hagiwara, M.: Retinoid derivative Tp80 exhibits anti-hepatitis C virus activity through restoration of GI-GPx expression Journal of Medical Virology. 2017.05; 89 (7): 1224-1234.

  30. Yoshida S, Nagai A, Uchida K, Hosoya T: Enhancing the Synthetic Utility of 3-Haloaryne Intermediates by their Efficient Generation from Readily Synthesizable #Iortho#IR-Iodoaryl Triflate-type Precursors. Chem Lett. 2017.05; 46 (5): 733-736. ( DOI )

  31. Hoang, H. N.; Nagashima, Y.; Mori, S.; Kagechika, H.; Matsuda, T.: CO2-expanded bio-based liquids as novel solvents for enantioselective biocatalysis Tetrahedron . 2017.05; 73 (20): 2984-2989.

  32. Sako Y, Ninomiya K, Okuno Y, Toyomoto M, Nishida A, Koike Y, Ohe K, Kii I, Yoshida S, Hashimoto N, Hosoya T, Matsuo M, Hagiwara M: Development of an orally available inhibitor of CLK1 for skipping a mutated dystrophin exon in Duchenne muscular dystrophy. Sci Rep. 2017.05; 7 46126. ( PubMed , DOI )

  33. Niwa T, Ochia H, Hosoya T: Copper-Catalyzed #Iipso#IR-Borylation of Fluoroarenes. ACS Catal. 2017.05; 7 (7): 4535-4541. ( DOI )

  34. Kobayashi K, Mizuguchi T, Hattori Y, Ohara N, Ninomiya R, Iida M, Ooe H, Yamazaki Y, Takata M, Tamamura H, Akaji K: Effects of Replacement and Addition of an Amino Acid Contained in a Cyclic Peptide Corresponding to a β-Hairpin Loop Sequence of Human EGF Receptor. J. Pept. Sci. 2017.04; ( DOI )

  35. Meguro T, Yoshida S, Hosoya T : Aromatic Azido-selective Reduction via the Staudinger Reaction Using Tri-#In#IR-butylphosphonium Tetrafluoroborate with Triethylamine. Chem Lett. 2017.04; 46 (4): 473-476. ( DOI )

  36. Perri, M.; Caroleo, Nannan M. C.; Gallelli, L. L.; De Sarro, G.; Kagechika, H.; Cione, E.: 9-cis Retinoic acid modulates myotrophin expression and its miR in physiological and pathophysiological cell models Experimental Cell Research. 2017.04; 354 25-30.

  37. Takuya Kobayakawa: Synthetic Studies on Chloroalkene Dipeptide Isosteres as Peptidomimetics 国立大学法人 東京医科歯科大学. 2017.03;

  38. Takano Hikaru, Narumi Tetsuo, Nomura Wataru, Tamamura Hirokazu: Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization JOURNAL OF ORGANIC CHEMISTRY. 2017.03; 82 (5): 2739-2744. ( PubMed , DOI )

  39. Uchida K, Yoshida S, Hosoya T: Three-Component Coupling of Triflyloxy-Substituted Benzocyclobutenones, Organolithium Reagents, and Arynophiles Promoted by Generation of Aryne via Carbon-Carbon Bond Cleavage. Org Lett. 2017.03; 19 (5): 1184-1187. ( PubMed , DOI )

  40. Tsuji, M.; Shudo, K.; Kagechika, H.: The receptor subtype selectivity of retinoid X and retinoic acid re-ceptors via quantum mechanics FEBS Open Bio. 2017.03; 7 391-396.

  41. Takano T, Narumi T, Nomura W, Tamamura H: Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization. J. Org. Chem. 2017.02; 82 (5): 2739-2744.

  42. Ochiai H, Uetake Y, Niwa T, Hosoya T: Rhodium-Catalyzed Decarbonylative Borylation of Aromatic Thioesters for Facile Diversification of Aromatic Carboxylic Acids. Angew Chem Int Ed. 2017.02; 56 (9): 2482-2486. ( PubMed , DOI )

  43. Yukihiro Itoh, Keisuke Aihara, Paolo Mellini, Toshifumi Tojo, Yosuke Ota, Hiroki Tsumoto, Viswas Raja Solomon, Peng Zhan, Miki Suzuki, Daisuke Ogasawara, Akira Shigenaga, Tsubasa Inokuma, Hidehiko Nakagawa, Naoki Miyata, Tamio Mizukami, Akira Otaka, Takayoshi Suzuki: Design, synthesis and biological evaluation of SNAIL1 peptide-based lysine specific demethylase 1 inhibitors Peptide Science 2016. 2017.02; 165-166.

  44. Tanaka T, Aoki T, Nomura W, Tamamura H : Bivalent 14-mer Peptide Ligands of CXCR4 with Polyproline Linkers with Anti-Chemotactic Activity against Jurkat Cells. J. Pept. Sci. 2017.01; ( DOI )

  45. Mizuguchi T, Ohashi N, Matsumoto D, Hashimoto C, Nomura W, Yamamoto N, Murakami T, Tamamura: Development of Anti-HIV Peptides Based on a Viral Capsid Protein. Biopolymers: Peptide Science. 2017.01; 108 (1): ( DOI )

  46. Morita T, Nishiyama Y, Yoshida S, Hosoya T: Facile Synthesis of Multisubstituted Benzo[#Ib#IR]furans via 2,3-Disubstituted 6,7-Furanobenzynes Generated from #Iortho#IR-Iodoaryl Triflate-type Precursors. Chem Lett. 2017.01; 46 (1): 118-121. ( DOI )

  47. Morita T, Yoshida S, Kondo M, Matsushita T, Hosoya T: Facile Diversification of Simple Benzo[#Ib#IR]thiophenes via Thienobenzyne Intermediates. Chem Lett. 2017.01; 46 (1): 81-84. ( DOI )

  48. Yoshida S, Nakajima H, Uchida K, Yano T, Kondo M, Matsushita T, Hosoya T: Reactions of Arynes with Sulfoximines: Formal Sulfinylamination vs. #IN#IR-Arylation. Chem Lett. 2017.01; 46 (1): 77-80. ( DOI )

  49. Oya, Y.; Mondal, A.; Rawangkan, A.; Umsumarng, S.; Iida, K.; Watanabe, T.; Kanno, M.; Suzuki, K.; Li, Z.; Kagechika, H.; Shudo, K.; Fujiki, H.; Suganuma, M.: Down-regulation of histone deacetylase 4, −5 and −6 as a mechanism of synergistic enhancement of apoptosis in human lung cancer cells treated with the combination of a synthetic retinoid, Am80 and green tea catechin Journol of Nutritional Biochemistry. 2017.01; 42 7-16.

  1. Yoshida S, Nakamura Y, Uchida K, Hazama Y, Hosoya T: Aryne Relay Chemistry en Route to Aminoarenes: Synthesis of 3-Aminoaryne Precursors via Regioselective Silylamination of 3-(Triflyloxy)arynes.. Org Lett. 2016.12; 18 (23): 6212-6215. ( PubMed , DOI )

  2. Ochiai H, Niwa T, Hosoya T: Stereoinversion of Stereocongested Carbocyclic Alcohols via Triflylation and Subsequent Treatment with Aqueous #IN#IR,#IN#IR-Dimethylformamide. Org Lett. 2016.12; 18 (23): 5982-5985. ( PubMed , DOI )

  3. Doi H, Sato K, Shindou H, Sumi K, Koyama H, Hosoya T, Watanabe Y, Ishii S, Tsukada H, Nakanishi K, Suzuki M: Blood-brain barrier permeability of ginkgolide: Comparison of the behavior of PET probes 7α-[#U18#URF]fluoro- and 10-#IO#IR-#Ip#IR-[#U11#URC]methylbenzyl ginkgolide B in monkey and rat brains. Bioorg Med Chem. 2016.11; 24 (21): 5148-5157. ( PubMed , DOI )

  4. Okamoto-Uchida Y, Yu R, Miyamura N, Arima N, Ishigami-Yuasa M, Kagechika H, Yoshida S, Hosoya T, Nawa M, Kasama T, Asaoka Y, Alois RW, Elling U, Penninger JM, Nishina S, Azuma N, Nishina H: The mevalonate pathway regulates primitive streak formation via protein farnesylation. Sci Rep. 2016.11; 6 37697. ( PubMed , DOI )

  5. Sumida Y, Sumida T, Hashizume D, Hosoya T: Preparation of Aryne-Nickel Complexes from #Iortho#IR-Borylaryl Triflates. Org Lett. 2016.11; 18 (21): 5600-5603. ( PubMed , DOI )

  6. Okamoto-Uchida, Y.; Yu, R.; Miyamura, N.; Arima, N.; Ishigami-Yuasa, M.; Kagechika, H.; Yoshida, S.; Hosoya, T.; Nawa, M.; Kasama, T.; Asaoka, Y.; Alois, R. W.; Elling, U.; Penninger, J. M.; Nishina, S.; Azuma, N.; Nishina, H.: The mevalonate pathway regulates primitive streak formation via protein farnesylation Science Reports. 2016.10; 6 37697.

  7. Yoshida S, Yano T, Nishiyama Y, Misawa Y, Kondo M, Matsushita T, Igawa K, Tomooka K, Hosoya T: Thiazolobenzyne: a versatile intermediate for multisubstituted benzothiazoles. Chem Commun. 2016.09; 52 (75): 11199-11202. ( PubMed , DOI )

  8. Tanaka T, Okuyama-Dobashi K, Murakami S, Chen W, Okamoto T, Ueda K, Hosoya T, Matsuura Y, Ryo A, Tanaka Y, Hagiwara M, Moriishi K: Inhibitory effect of CDK9 inhibitor FIT-039 on hepatitis B virus propagation. Antiviral Res. 2016.09; 133 156-164. ( PubMed , DOI )

  9. Kinoshita, M.; Negishi, M.; Sakai, H.; Hirano, T.; Mori, S.; Fujii, S.; Kagechika, H.; Tanatani, A.: Development of 6-Arylcoumarins as Nonsteroidal Progesterone Antagonists. Structure-activity Relationships and Fluorescence Properties Bioorganic & Medicinal Chemistry. 2016.09; 24 (21): 5602-5610.

  10. Yamada, A.; Kazui, Y.; Yoshioka, H.; Tanatani, A.; Mori, S.; Kagechika, H.; Fujii, S. : Development of N-(4-Phenoxyphenyl)benzenesulfonamide Derivatives as Novel Nonsteroidal Progesterone Receptor Antagonists ACS Medicinal Chemistry Letters. 2016.09; 7 (12): 1028-1033.

  11. Takuya Kobayakawa, Hirokazu Tamamura: Efficient synthesis of Xaa-Gly type (Z)-chloroalkene dipeptide isosteres via organocuprate mediated reduction Tetrahedron. 2016.08; 72 (32): 4968-4971. ( DOI )

  12. Kobayakawa Takuya, Tamamura Hirokazu: Development of synthetic methodology of chloroalkene-type dipeptide isosteres for peptidomimetics ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY. 2016.08; 252

  13. Mitsuhiro Eto, Naoto Naruse, Kyohei Morimoto, Kosuke Yamaoka, Kohei Sato, Kohei Tsuji, Tsubasa Inokuma, Akira Shigenaga, Akira Otaka: Development of an Anilide-Type Scaffold for the Thioester Precursor N-Sulfanylethylcoumarinyl Amide. Org. Lett.. 2016.08; 18 (17): 4416-4419. ( PubMed , DOI )

  14. Controlled Generation of 3-Triflyloxyarynes. Synthesis. 2016.08; 48 (23): 4099-4109. ( DOI )

  15. Yoshida S, Shimomori K, Kim Y, Hosoya T: Single C-F Bond Cleavage of Trifluoromethylarenes with an #Iortho#IR-Silyl Group. Angew Chem Int Ed Engl. 2016.08; 55 (35): 10406-10409. ( PubMed , DOI )

  16. Yokoo, H.; Ohsaki, A.; Kagechika, H.; Hirano T.: Structural development of canthin-5,6-dione moiety as a fluorescent dye and its application to novel fluorescent sensors Tetrahedron . 2016.08; 72 5872-5879.

  17. Yoshida S, Morita T, Hosoya T: Synthesis of Diverse Benzotriazoles from Aryne Precursors Bearing an Azido Group via Inter- and Intramolecular Cycloadditions. Chem Lett. 2016.07; 45 (7): 726-728. ( DOI )

  18. Fujiwara, T.; Ohira, K.; Urushibara, K.; Ito, A.; Yoshida, M.; Kanai, M.; Tanatani, A.; Kagechika, H.; Hirano, T.: Steric structure–activity relationship of cyproheptadine derivatives as inhibitors of histone methyltransferase Set7/9 Bioorganic & Medicinal Chemistry. 2016.07; 24 4318-4323.

  19. Uetake Y, Niwa T, Hosoya T: Rhodium-Catalyzed #Iipso#IR-Borylation of Alkylthioarenes via C-S Bond Cleavage. Org Lett. 2016.06; 18 (11): 2758-2761. ( PubMed , DOI )

  20. Hirano, T.; Noji, Y.; Shiraishi, T.; Ishigami-Yuasa, M.; Kagechika, H.: Development of an “OFF-ON-OFF” fluorescent pH sensor suitable for the study of intracellular pH Tetrahedron . 2016.06; 72 4925-4930.

  21. Nagashima, S.; Maruyama, J.; Kawano, S.; Iwasa, H.; Nakagawa, K.; Ishigami-Yuasa, M.; Kagechika, H.; Nishina, H.; Hata, Y.: Validation of the chemical compound library screening for TAZ inhibitors by use of green fluorescence protein-fused TAZ Cancer Science. 2016.06; 107 (6): 791-802.

  22. Sasaki Ikuo, Ikeda Toshiki, Amou Tatsunosuke, Taguchi Jumpei, Ito Hajime, Ishiyama Tatsuo: Regioselective C-H Borylation of Heteroaromatic Aldimines with Iridium Complexes SYNLETT. 2016.06; 27 (10): 1582-1586. ( DOI )

  23. Sasaki Ikuo, Taguchi Jumpei, Doi Hana, Ito Hajime, Ishiyama Tatsuo: Iridium(I)-catalyzed C-H Borylation of alpha,beta-Unsaturated Esters with Bis(pinacolato)diboron CHEMISTRY-AN ASIAN JOURNAL. 2016.05; 11 (9): 1400-1405. ( DOI )

  24. Takemoto, Y.; Ito, A.; Niwa, H.; Okamura, M.; Fujiwara, T.; Hirano, T.; Handa, N.; Umehara, T.; Sonoda, T.; Ogawa, K.; Tariq, M.; Nishino, N.; Dan, S.; Kagechika, H.; Yamori, T.; Yokoyama, S.; Yoshida, M.: Identification of Cyproheptadine as an Inhibitor of SET Domain Containing Lysine Methyltransferase 7/9 (Set7/9) That Regulates Estrogen-Dependent Transcription Journol of Medicinal Chemistry. 2016.04; 59 (8): 3650-3660.

  25. Takuya Kobayakawa, Tetsuo Narumi, Hirokazu Tamamura: Stereoselective Synthesis of Chloroalkene Dipeptide Isosteres Utilizing Organocopper Reagents PEPTIDE SCIENCE 2015. 2016.03; 97-98.

  26. Persaud, S. D.; Park, S. W.; Ishigami-Yuasa, M.; Koyano-Nakagawa, N.;, Kagechika, H.; Wei, L.-N.: All trans-retinoic acid analogs promote cancer cell apoptosis through non-genomic Crabp1 mediating ERK1/2 phosphorylation Science Reports. 2016.03; 6 22396.

  27. Study of Ligand Binding Selectivity of Histone Deacetylases by Replica-Exchange Umbrella Sampling Molecular Dynamics Simulations 2016.02; 110 (3): 544A-545A.

  28. Tomabechi Y, Hosoya T, Ehara H, Sekine S, Shirouzu M, Inouye S: Crystal structure of nanoKAZ: The mutated 19 kDa component of #IOplophorus#IR luciferase catalyzing the bioluminescent reaction with coelenterazine. Biochem Biophys Res Commun. 2016.01; 470 (1): 88-93. ( PubMed , DOI )

  29. Tsukada, H.; Kawabe, H.; Ohtaka, A.; Saito, Y.: Okamoto, Y.: Tori, M.; Kagechika, H.; Hirota, H.; Gong, X.; Kuroda, C.; Ohsaki, A.: Two new diterpenoids from Salvia przewarskii Natural Product Communications. 2016.01; 11 (2): 159-161.

  30. Mizuguchi T, Harada S, Miura T, Ohashi N, Narumi T, Mori H, Irahara Y, Yamada Y, Nomura W, Matsushita S, Yoshimura K, Tamamura H: A Minimally Cytotoxic CD4 Mimic as an HIV Entry Inhibitor Bioorg. Med. Chem. Lett . 2016; 2 (26): 397-400.

  31. Isao Kii, Yuto Sumida, Toshiyasu Goto, Rie Sonamoto, Yukiko Okuno, Suguru Yoshida, Tomoe Kato-Sumida, Yuka Koike, Minako Abe, Yosuke Nonaka, Teikichi Ikura, Nobutoshi Ito, Hiroshi Shibuya, Takamitsu Hosoya, Masatoshi Hagiwara: Selective inhibition of the kinase DYRK1A by targeting its folding process. Nat Commun. 2016; 7 11391. ( PubMed , DOI )

  32. Takano H, Narumi T, Nomura W, Tamamura H: Microwave-Assisted Synthesis of Azacoumarin Fluorophores and the Fluorescence Characterization J. Org. Chem. 2016; in press

  33. Nakamura T, Campbell J.R, Moore A.R, Otsu S, Aikawa H, Tamamura H, Mitsuya H: Development and Validation of a Cell-based Assay System to Assess Human Immunodeficiency Virus Type 1 Integrase Multimerization J. Virol. Methods. 2016; 236 196-206.

  34. Nomura W, Mizuguchi T & Tamamura H: Multimerized HIV-gp41-derived Peptides as Fusion Inhibitors and Vaccines Biopolymers: Peptide Science. 2016; 106 (4): 622-628.

  35. Ohashi N, Harada S, Mizuguchi T, Irahara Y, Yamada Y, Kotani M, Nomura W, Matsushita S, Yoshimura K, Tamamura H: Small Molecular CD4 Mimics Containing Mono-cyclohexyl Moieties as HIV Entry Inhibitors. ChemMedChem a joint special issue with ChemBioChem: Protein–Protein Interactions. 2016; 11 (8): 940-946.

  36. Hiramatsu K, Tamamura H: A Mild Method for the Direct Fluorination of Pyrroles by Using a Lipophilic Anionic Phase-Transfer Catalyst. Eur. J. Org. Chem. 2016; 21 3491-3494.

  37. Toyama K, Mizuguchi T, Nomura W, Tamamura H: Functional Evaluation of Fluorescein-Labeled Derivatives of a Peptide Inhibitor of the EGF Receptor Dimerization Bioorg. Med. Chem. 2016; 24 (16): 3406-3412.

  38. Abduelmula A, Huang R, Pu Q, Tamamura H, Puopolo G. M & Saberi B. B: SDF-1 Controls the Muscle and Blood Vessel Formation of the Somite. Int. J. Dev. Biol. 2016; 60(1-2-3) (29-38):

  1. Yoshida S, Sugimura Y, Hazama Y, Nishiyama Y, Yano T, Shimizu S, Hosoya T: A mild and facile synthesis of aryl and alkenyl sulfides #Ivia#IR copper-catalyzed deborylthiolation of organoborons with thiosulfonates. Chem Commun. 2015.12; 51 (93): 16613-16616. ( PubMed , DOI )

  2. Shrestha, R.; Tatsukawa, H.; Shrestha, R.; Ishibashi, N.; Matsuura, T.; Kagechika, H.; Kose, S.; Hitomi, K.; Imamoto, N.; Kojima, S.: Molecular mechanism by which acyclic retinoid induces nuclear localization of transglutaminase 2 in human hepatocellular carcinoma cells. Cell Death & Disease. 2015.12; 6 e2002. ( DOI )

  3. Okamoto M, Hidaka A, Toyama M, Hosoya T, Yamamoto M, Hagiwara M, Baba M: Selective inhibition of HIV-1 replication by the CDK9 inhibitor FIT-039. Antiviral Res. 2015.11; 123 1-4. ( PubMed , DOI )

  4. Yoshida S, Yano T, Misawa Y, Sugimura Y, Igawa K, Shimizu S, Tomooka K, Hosoya T: Direct thioamination of arynes via reaction with sulfilimines and migratory #IN#IR-arylation. J Am Chem Soc. 2015.11; 137 (44): 14071-14074. ( PubMed , DOI )

  5. Niwa T, Ochiai H, Watanabe Y, Hosoya T: Ni/Cu-Catalyzed Defluoroborylation of Fluoroarenes for Diverse C-F Bond Functionalizations. J Am Chem Soc. 2015.11; 137 (45): 14313-14318. ( PubMed , DOI )

  6. Yoshida S, Hosoya T: The Renaissance and Bright Future of Synthetic Aryne Chemistry. Chem Lett. 2015.11; 44 (11): 1450-1460. ( DOI )

  7. Saito-Hakoda, A.; Uruno, A.; Yokoyama, A.; Shimizu, K.; Parvin, R.; Kudo, M.; Saito-Ito, T.; Sato, I.; Kogure, N.; Suzuki, D.; Shimada, H.; Yoshikawa, T .; Fujiwara, I.; Kagechika, H.; Iwasaki, Y.; Kure, S.; Ito, S.; Sugawara, A.: Effects of RXR Agonists on Cell Proliferation/Apoptosis and ACTH Secretion/Pomc Expression Plos ONE. 2015.11; 10 e0141960. ( DOI )

  8. Yu. R.: Miyamura, N.; Okamoto-Uchida, Y.; Arima, N.; Ishigami-Yuasa, M.; Kagechika, H.; Nishina, H.: A Modified Murine Embryonic Stem Cell Test for Evaluating the Teratogenic Effects of Drugs on Early Embryogenesis Plos ONE. 2015.11; 10 e0145286. ( DOI )

  9. Wataru Nomura, Takaaki Mizuguchi & Hirokazu Tamamura: Multimerized HIV-gp41-derived Peptides as Fusion Inhibitors and Vaccines Biopolymers: Peptide Science. 2015.11; ( DOI )

  10. Yoshida S, Shimomori K, Nonaka T, Hosoya T: Facile Synthesis of Diverse Multisubstituted #Iortho#IR-Silylaryl Triflates via C–H Borylation. Chem Lett. 2015.10; 44 (10): 1324-1326. ( DOI )

  11. Kohei Tsuji, Kosuke Tanegashima, Kohei Sato, Ken Sakamoto, Akira Shigenaga, Tsubasa Inokuma, Takahiko Hara, Akira Otaka: Efficient one-pot synthesis of CXCL14 and its derivative using an N-sulfanylethylanilide peptide as a peptide thioester equivalent and their biological evaluation. Bioorg. Med. Chem.. 2015.09; 23 (17): 5909-5914. ( PubMed , DOI )

  12. Chiharu Mizuguchi, Fuka Ogata, Shiho Mikawa, Kohei Tsuji, Teruhiko Baba, Akira Shigenaga, Toshinori Shimanouchi, Keiichiro Okuhira, Akira Otaka, Hiroyuki Saito: Amyloidogenic Mutation Promotes Fibril Formation of the N-terminal Apolipoprotein A-I on Lipid Membranes. J. Biol. Chem.. 2015.08; 290 (34): 20947-20959. ( PubMed , DOI )

  13. Yusuke Tsuda, Akira Shigenaga, Kohei Tsuji, Masaya Denda, Kohei Sato, Keisuke Kitakaze, Takahiro Nakamura, Tsubasa Inokuma, Kohji Itoh, Akira Otaka: Development of a Chemical Methodology for the Preparation of Peptide Thioesters Applicable to Naturally Occurring Peptides Using a Sequential Quadruple Acyl Transfer System. ChemistryOpen. 2015.08; 4 (4): 448-452. ( PubMed , DOI )

  14. Sonamoto R, Kii I, Koike Y, Sumida Y, Kato-Sumida T, Okuno Y, Hosoya T, Hagiwara M: Identification of a DYRK1A Inhibitor that Induces Degradation of the Target Kinase using Co-chaperone CDC37 fused with Luciferase nanoKAZ. Sci Rep. 2015.08; 5 12728. ( PubMed , DOI )

  15. Hosoya T, Iimori R, Yoshida S, Sumida Y, Sahara-Miura Y, Sato J, Inouye S: Concise Synthesis of #Iv#IR-Coelenterazines. Org Lett. 2015.08; 17 (15): 3888-3891. ( PubMed , DOI )

  16. Masaki S, Kii I, Sumida Y, Kato-Sumida T, Ogawa Y, Ito N, Nakamura M, Sonamoto R, Kataoka N, Hosoya T, Hagiwara M: Design and synthesis of a potent inhibitor of class 1 DYRK kinases as a suppressor of adipogenesis. Bioorg Med Chem. 2015.08; 23 (15): 4434-4441. ( PubMed , DOI )

  17. Morooka S, Hoshina M, Kii I, Okabe T, Kojima H, Inoue N, Okuno Y, Denawa M, Yoshida S, Fukuhara J, Ninomiya K, Ikura T, Furuya T, Nagano T, Noda K, Ishida S, Hosoya T, Ito N, Yoshimura N, Hagiwara M: Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice. Mol Pharmacol. 2015.08; 88 (2): 316-325. ( PubMed , DOI )

  18. Kikuchi E, Mori T, Zeniya M, Isobe K, Ishigami-Yuasa M, Fujii S, Kagechika H, Ishihara T, Mizushima T, Sasaki S, Sohara E, Rai T, Uchida S: Discovery of novel SPAK inhibitors that block WNK kinase signaling to cation chloride transporters. J Am Soc Nephrol. 2015.07; 26 (7): 1525-1536. ( PubMed , DOI )

  19. Yoshida S, Hazama Y, Sumida Y, Yano T, Hosoya T: An Alternative Method for Generating Arynes from #Iortho#IR-Silylaryl Triflates: Activation by Cesium Carbonate in the Presence of a Crown Ether. Molecules. 2015.06; 20 (6): 10131-10140. ( PubMed , DOI )

  20. Sasaki Ikuo, Taguchi Jumpei, Hiraki Shotaro, Ito Hajime, Ishiyama Tatsuo: Catalyst-Controlled Regiodivergent CH Borylation of Multifunctionalized Heteroarenes by Using Iridium Complexes CHEMISTRY-A EUROPEAN JOURNAL. 2015.06; 21 (25): 9236-9241. ( DOI )

  21. Yoshida S, Karaki F, Uchida F, Hosoya T: Generation of cycloheptynes and cyclooctynes #Ivia#IR a sulfoxide-magnesium exchange reaction of readily synthesized 2-sulfinylcycloalkenyl triflates. Chem Commun. 2015.05; 51 (42): 8745-8748. ( PubMed , DOI )

  22. Yoshida S, Uchida K, Hosoya T: Generation of Arynes Using Trimethylsilylmethyl Grignard Reagent for Activation of #Iortho#IR-Iodoaryl or #Iortho#IR-Sulfinylaryl Triflates. Chem Lett. 2015.05; 44 (5): 691-693. ( DOI )

  23. Takuya Kobayakawa, Tetsuo Narumi, Hirokazu Tamamura: Remote Stereoinduction in the Organocuprate-Mediated Allylic Alkylation of Allylic gem-Dichlorides: Highly Diastereoselective Synthesis of (Z)-Chloroalkene Dipeptide Isosteres. Organic Letters. 2015.05; 17 (10): 2302-2305. ( PubMed , DOI )

  24. Takuya Kobayakawa, Tetsuo Narumi, Hirokazu Tamamura: Development of Efficient Synthetic Methodologies of Chloroalkene Dipeptide Isosteres PEPTIDE SCIENCE 2014. 2015.03; 13-14.

  25. Yuki Takechi-Haraya, Kento Tanaka, Kohei Tsuji, Yasuo Asami, Hironori Izawa, Akira Shigenaga, Akira Otaka, Hiroyuki Saito, Kohsaku Kawakami: Molecular complex composed of β-cyclodextrin-grafted Chitosan and pH-sensitive amphipathic peptide for enhancing cellular cholesterol efflux under acidic pH. Bioconjug. Chem.. 2015.03; 26 (3): 572-581. ( PubMed , DOI )

  26. Yoshida M, Kataoka N, Miyauchi K, Ohe K, Iida K, Yoshida S, Nojima T, Okuno Y, Onogi H, Usui T, Takeuchi A, Hosoya T, Suzuki T, Hagiwara M: Rectifier of aberrant mRNA splicing recovers tRNA modification in familial dysautonomia. Proc Natl Acad Sci USA. 2015.03; 112 (9): 2764-2769. ( PubMed , DOI )

  27. Nomura W, Koseki T, Ohashi N, Mizuguchi T, Tamamura H: Trivalent Lignds for CXCR4 Bearing Polyproline Linkers Show Specific Recognition for Cells with Increased CXCR4 Expression. Org Biomol Chem. 2015; 32 (13): 8734-8739.

  28. Mizuguchi T, Ohashi N, Nomura W, Komoriya M, Hashimoto C, Yamamoto N, Murakami T, Tamamura H: Anti-HIV Screening for Cell-Penetrating Peptides Using Chloroquine and Identification of Anti-HIV Peptides Derived from Matrix Proteins. Bioorg Med Chem. 2015; 15 (23): 4423-4427.

  29. Nomura W, Ohashi N, Mori A, Tamamura H: An In-cell Fluorogenic Tag-probe System for Protein Dynamics Imaging Enabled by Cell-Penetrating Peptides. Bioconjugate Chem. 2015; 6 (26): 1080-1085.

  30. Shiraishi, T.; Kagechika, H.; Hirano, T.: 6-Arylcoumarins: versatile scaffolds for fluorescent sensors New Journal of Chemistry. 2015; 39 8389-8396. ( DOI )

  31. Tsuji, M.; Shudo, K.; Kagechika, H.: Docking simulations suggest that all-trans retinoic acid could bind to retinoid X receptors Journal of Computer Aided Molecular Design. 2015; 29 975-988. ( DOI )

  32. Kawano, S.; Maruyama, J.; Nagashima, S.; Inami, K.; Qiu, W.; Iwasa, H.; Nakagawa, K.; Ishigami-Yuasa, M.; Kagechika, H.; Nishina, H.; Hata, Y.: A cell-based screening for TAZ activators identifies ethacridine, a widely used antiseptic and abortifacient, as a compound that promotes dephosphorylation of TAZ and inhibits adipogenesis in C3H10T1/2 cells The Journal of Biochemistry. 2015; 158 413-420. ( DOI )

  33. Brun, P.-J., Grijalva, A., Rausch, R., Watson, E., Yuen, J. J., Das, B. C., Shudo, K., Kagechika, H., Leibel, R. L., Blaner, W. S.: Retinoic acid receptor signaling is required to maintain glucose-stimulated insulin secretion and β-cell mass FASEB Journal. 2015; 26 671-683. ( DOI )

  34. Mori, S., Takeuchi, Y., Tanatani, A., Kagechika, H., Fujii, S.: Development of 1,3-diphenyladamantane derivatives as nonsteroidal progesterone receptor antagonists Bioorganic Medicinal Chemistry. 2015; 23 803-809. ( DOI )

  35. Nishiyama, S.; Urushibara, K.; Masu, H.; Azumaya, I.; Kagechika, H. Tanatani, A.: Conformational and chiral properties of cyclic-tri(N-methyl-meta-benzamide) bearing amidino groups Chirality. 2015; 27 487-491. ( DOI )

  36. Inoue, K.; Urushibara, K.; Kanai, M.; Yura, K.; Fujii, S.; Ishigami-Yuasa, M.; Hashimoto, Y.; Mori, S.; Kawachi, E.; Matsumura, M.; Hirano, T.; Kagechik, H.; Tanatani, A.: Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists European Journal of Medicinal Chemistry. 2015; 102 310-319. ( DOI )

  37. Kodaka, M.; Yang, Z.; Nakagawa, K.; Maruyama, J.; Xu, X.; Sarkar, A.; Ichimura, A.; Nasu, Y.; Ozawa, T.; Iwasa, H.; Ishigami-Yuasa, M.; Ito, S.; Kagechika, H.; Hata, Y.: A new cell-based assay to evaluate myogenesis in mouse myoblast C2C12 cells Experimental Cell Research. 2015; 336 171-181. ( DOI )

  38. Qin, X.-Y.; Fujii, S.; Shimizu, A.; Kagechika, H.; KOJIMA, S.: Carboxylic derivatives of vitamin K2 inhibit hepatocellular carcinoma cell growth through caspase/transglutaminase-related signaling pathways Journal of Nutritional Science and Vitaminology. 2015; 61 285-290.

  39. Fujii, S.; Shimizu, A.; Takeda, N.; Oguchi, K.; Katsurai, T.; Shirakawa, H.; Komai, M.; Kagechika, H.: Systematic synthesis and anti-inflammatory activity of ω-carboxylated menaquinone derivatives - Investigations on identified and putative vitamin K2 metabolites - Bioorganic Medicinal Chemistry. 2015; 23 2344-2352.

  40. Takano H, Narumi T, Nomura W, Furuta T, Tamamura H: Utilization of the Heavy Atom Effect for the Development of a Photosensitive 8-Azacoumarin-type Photolabile Protecting Group Org Lett. 2015; 21 (17): 5372-5375.

  41. Nomura W, Aikawa H, Taketomi S, Tanabe M, Mizuguchi T, Tamamura H: Exploration of Labeling of Near Infrared Dyes on the Polyproline Linker for Bivalent-Type CXCR4 Ligands Bioorg Med Chem. 2015; 21 (23): 6967-6973.

  1. Yoshida S, Uchida K, Igawa K, Tomooka K, Hosoya T: An efficient generation method and remarkable reactivities of 3-triflyloxybenzyne. Chem Commun (Camb.). 2014.11; 50 (95): 15059-15062. ( PubMed , DOI )

  2. Xu F, Peng L, Shinohara K, Morita T, Yoshida S, Hosoya T, Orita A, Otera J: Substituted 5,6,11,12-Tetradehydrodibenzo[a,e]cyclooctenes: Syntheses, Properties, and DFT Studies of Substituted Sondheimer-Wong Diynes. J Org Chem. 2014.11; 79 (23): 11592-11608. ( PubMed , DOI )

  3. Sumida Y, Harada R, Kato-Sumida T, Johmoto K, Uekusa H, Hosoya T: Boron-Selective Biaryl Coupling Approach to Versatile Dibenzoxaborins and Application to Concise Synthesis of Defucogilvocarcin M. Org Lett. 2014.11; 16 (23): 6240-6243. ( PubMed , DOI )

  4. Yoshida S, Nonaka T, Morita T, Hosoya T: Modular synthesis of bis- and tris-1,2,3-triazoles by permutable sequential azide-aryne and azide-alkyne cycloadditions. Org Biomol Chem. 2014.10; 12 (38): 7489-7493. ( PubMed , DOI )

  5. Yoshida S, Hatakeyama Y, Johmoto K, Uekusa H, Hosoya T: Transient protection of strained alkynes from click reaction via complexation with copper. J Am Chem Soc. 2014.10; 136 (39): 13590-13593. ( PubMed , DOI )

  6. Inouye S, Sato J-i, Sahara-Miura Y, Hosoya T, Suzuki T: Unconventional secretion of the mutated 19 kDa protein of Oplophorus luciferase (nanoKAZ) in mammalian cells. Biochem Biophys Res Commun. 2014.08; 450 (4): 1313-1319. ( PubMed , DOI )

  7. Yamamoto M, Onogi H, Kii I, Yoshida S, Iida K, Sakai H, Abe M, Tsubota T, Ito N, Hosoya T, Hagiwara M: CDK9 inhibitor FIT-039 prevents replication of multiple DNA viruses. J Clin Invest. 2014.08; 124 (8): 3479-3488. ( PubMed , DOI )

  8. Suzuki M, Doi H, Koyama H, Zhang Z, Hosoya T, Onoe H, Watanabe Y: Pd0-mediated rapid cross-coupling reactions, the rapid C-[11C]methylations, revolutionarily advancing the syntheses of short-lived PET molecular probes. Chem Rec. 2014.06; 14 (3): 516-541. ( PubMed , DOI )

  9. Yoshida S, Misawa Y, Hosoya T: Formal C–H-Azidation Based Shortcut to Diazido Building Blocks for the Versatile Preparation of Photoaffinity Labeling Probes. Eur J Org Chem. 2014.05; (19): 3991-3995. ( DOI )

  10. Takahashi K, Hosoya T, Onoe K, Doi H, Nagata H, Hiramatsu T, Li XL, Watanabe Y, Wada Y, Takashima T, Suzuki M, Onoe H, Watanabe Y: 11C-Cetrozole: An Improved C-11C-Methylated PET Probe for Aromatase Imaging in the Brain. J Nucl Med. 2014.03; 55 (5): 852-857. ( PubMed , DOI )

  11. Sumi K, Inoue Y, Nishio M, Naito Y, Hosoya T, Suzuki M, Hidaka H: IOP-lowering effect of isoquinoline-5-sulfonamide compounds in ocular normotensive monkeys. Bioorg Med Chem Lett. 2014.02; 24 (3): 831-834. ( PubMed , DOI )

  12. Inouye S, Sato J, Sahara-Miura Y, Yoshida S, Hosoya T: Luminescence enhancement of the catalytic 19kDa protein (KAZ) of Oplophorus luciferase by three amino acid substitutions. Biochem Biophys Res Commun. 2014.02; 445 (1): 157-162. ( PubMed , DOI )

  13. Emi Adachi, Asako Kosaka, Kohei Tsuji, Chiharu Mizuguchi, Hiroyuki Kawashima, Akira Shigenaga, Kohjiro Nagao, Kenichi Akaji, Akira Otaka, Hiroyuki Saito: The extreme N-terminal region of human apolipoprotein A-I has a strong propensity to form amyloid fibrils. FEBS Lett.. 2014.01; 588 (3): 389-394. ( PubMed , DOI )

  14. Yoshida S, Uchida K, Hosoya T: Generation of arynes triggered by sulfoxide-metal exchange reaction of ortho-sulfinylaryl triflates. Chem Lett. 2014; 43 (1): 116-118. ( DOI )

  15. Fujii, S.; Kano, A.; Songkram, C.; Masuno, H.; Taoda, Y.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H.: Synthesis and structure-activity relationship of p-carborane-based non-secosteroidal vitamin D analogs. Bioorganic Medicinal Chemistry. 2014; 22 1227-1235. ( DOI )

  16. Uruno, A.; Saito-Hakoda, A.; Yokoyama, A.; Kogure, N.; Matsuda, K.; Parvin, R.; Shimizu, K.; Sato, I.; Kudo, M.; Yoshikawa, T.; Kagechika, H.; Iwasaki, Y.; Ito, S.; Sugawara, A.: Retinoic acid receptor-α up-regulates proopiomelanocortin gene expression in AtT20 corticotroph cells. Endocrine Journol. 2014; 61 1105-1114. ( DOI )

  17. Tetsuo Narumi, Hikaru Takano, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta & Hirokazu Tamamura: Isostere-Based Design of 8-Azacoumarin-type Photolabile Protecting Groups: A Hydrophilicity Increasing Strategy for Coumarin-4-ylmethyls. Org. Lett.,. 2014; 16 (4): 1184-1187.

  18. Jun Yamamoto, Masaya Denda, Nami Maeda, Miku Kita, Chiaki Komiya, Tomohiro Tanaka, Wataru Nomura, Hirokazu Tamamura, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka: Development of a Traceable Linker Containing a Thiol-responsive Amino Acid for the Enrichment and Selective Labelling of Target Proteins. Org. Biomol. Chem.,. 2014; 12 (23): 3821-3826.

  19. Hikaru Takano, Tetsuo Narumi, Nami Ohashi, Akinobu Suzuki, Toshiaki Furuta, Wataru Nomura & Hirokazu Tamamura: Development of the 8-Aza-3-bromo-7-hydroxycoumarin-4-ylmethyl Group as a New Entry of Photolabile Protecting Groups. Tetrahedron, . 2014; 70 (29): 4400-4404.

  20. Jun Yamamoto, Nami Maeda, Chiaki Komiya, Tomohiro Tanaka, Masaya Denda, Koji Ebisuno, Wataru Nomura, Hirokazu Tamamura, Youichi Sato, Aiko Yamauchi, Akira Shigenaga & Akira Otaka: Development of a Fluoride-responsive Amide Bond Cleavage Device that is Potentially Applicable to a Traceable Linker. Tetrahedron,. 2014; 70 (34): 5122-5127.

  21. Nami Ohashi, Wataru Nomura, Natsuki Minato & Hirokazu Tamamura : Screening for Protein Kinase C Ligands Using Fluorescence Resonance Energy Transfer. Chem. Pharm. Bull., . 2014; 62 (10): 1019-1025.

  22. Fujii, S.; Sekine, R.; Kano, A.; Masuno, H.; Songkram, C.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H.: Structural development of p-carborane-based potent non-secosteroidal vitamin D analogs Bioorganic Medicinal Chemistry. 2014; 22 5891-5901. ( DOI )

  23. Fujii, S.; Nakano, E.; Yanagid, N.; Mori, S.; Masuno, H.; Kagechika, H.: Development of p-carborane-based nonsteroidal progesterone receptor antagonists Bioorganic Medicinal Chemistry. 2014; 22 5329-5337. ( DOI )

  24. Fujii, S.; Yamada, A.; Nakano, E.; Takeuchi, Y.; Mori, S.; Masuno, H.; Kagechika, H.: Design and synthesis of nonsteroidal progesterone receptor antagonists based on C,C’-diphenylcarborane scaffold as a hydrophobic pharmacophore Europian Journol of Medicinal Chemistry. 2014; 84 264-277. ( DOI )

  25. Fujii, S.; Kano, A.; Masuno, H.; Songkram, C.; Kawachi, E.; Hirano, T.; Tanatani, A.; Kagechika, H.: Design and synthesis of tetraol derivatives of　 1,12-dicarba-closo-dodecaborane as non-secosteroidal vitamin D analogs Bioorganic Medicinal Chemistry Letters. 2014; 24 4515-4519. ( DOI )

  26. Yang, Z. Y.; Nakagawa, K.; Sarkar, A.; Maruyama, J.; Iwasa, H.; Bao, Y. J.; Ishigami-Yuasa, M.; Ito, S.; Kagechika, H.; Hata, S.; Nishina, H.; Abe, S.; Kitagawa, M.; Hata, Y.: Screening with a Novel Cell-Based Assay for TAZ Activators Identifies a Compound That Enhances Myogenesis in C2C12 Cells and Facilitates Muscle Repair in a Muscle Injury Model Molecular Cellular Biology. 2014; 34 1607-1621.

  27. Fujii, S.; Kobayashi, T.; Nakatsu, A.; Miyazawa, H.; Kagechika, H.: Synthesis and Structure–Activity Relationship Study of Triazine-Based Inhibitors of the DNA Binding of NF-κB Chemical Pharmaceutical Bulletin. 2014; 62 700-708. ( DOI )

  28. Ma, F.; Liu, S.-Y.; Razani, B.; Arora, N.; Li, B.; Kagechika, H.; Tontonoz, P.; Nunez, V.; Ricote, M.; Cheng, G.: Retinoid X receptor a attenuates host antiviral response by suppressing type I interferon Nature Communication. 2014; 5 5494. ( DOI )

  29. Mori, S.; Takagaki, R.; Fujii, S.; Matsumura, M.; Tanatani, A.; Kagechika, H.: Lipase-catalyzed asymmetric acylation of boron cluster-containing secondary alcohols Tetrahedron Asymmetry. 2014; 25 1505-1512. ( DOI )

  30. Canavan, M.; McCarthy, C.; Ben Larbi, N.; Dowling, J. K.; Collins, L.; O'Sullivan, F.; Hurley, G.; Murphy, C.; Quinlan, A.; Moloney, G.; Darby, T.; MacSharry, J.; Kagechika, H.; Moynagh, P.; Melgar, S.; Loscher, C. E.: Activation of liver X receptor suppresses the production of the IL-12 family of cytokines by blocking nuclear translocation of NF-kappa Bp50 Innate Immunology. 2014; 20 675-687. ( DOI )

  31. Shiraishi, T.; Saito, T.; Kagechika, H.; Hirano, T.: Development of a novel fluorescent sensor to detect a specific range of pH Tetrahedron Letters. 2014; 55 6784-6786. ( DOI )

  1. Kosuke Tanegashima#, Kohei Tsuji#, Kenji Suzuki, Akira Shigenaga, Akira Otaka, Takahiko Hara (#Equally contributed): Dimeric peptides of the C-terminal region of CXCL14 function as CXCL12 inhibitors. FEBS Lett.. 2013.11; 587 (23): 3770-3775. ( PubMed , DOI )

  2. Tanaka K, Nakamoto Y, Siwu ER, Pradipta AR, Morimoto K, Fujiwara T, Yoshida S, Hosoya T, Tamura Y, Hirai G, Sodeoka M, Fukase K: Development of bis-unsaturated ester aldehydes as amino-glue probes: sequential double azaelectrocyclization as a promising strategy for bioconjugation. Org Biomol Chem. 2013.11; 11 (42): 7326-7333. ( PubMed , DOI )

  3. Miyajima M, Kusuhara H, Takahashi K, Takashima T, Hosoya T, Watanabe Y, Sugiyama Y: Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system. J Pharm Sci. 2013.09; 102 (9): 3309-3319. ( PubMed , DOI )

  4. Inouye S, Sato J, Sahara-Miura Y, Yoshida S, Kurakata H, Hosoya T: C6-Deoxy coelenterazine analogues as an efficient substrate for glow luminescence reaction of nanoKAZ: the mutated catalytic 19 kDa component of Oplophorus luciferase. Biochem Biophys Res Commun. 2013.07; 437 (1): 23-28. ( PubMed , DOI )

  5. Kosuke Tanegashima, Kenji Suzuki, Yuki Nakayama, Kohei Tsuji, Akira Shigenaga, Akira Otaka, Takahiko Hara: CXCL14 is a natural inhibitor of the CXCL12-CXCR4 signaling axis. FEBS Lett.. 2013.06; 587 (12): 1731-1735. ( PubMed , DOI )

  6. Sumida Y, Kato T, Hosoya T: Generation of arynes via ate complexes of arylboronic esters with an ortho-leaving group. Org Lett. 2013.06; 15 (11): 2806-2809. ( PubMed , DOI )

  7. Inouye S, Sahara-Miura Y, Sato J, Iimori R, Yoshida S, Hosoya T: Expression, purification and luminescence properties of coelenterazine-utilizing luciferases from Renilla, Oplophorus and Gaussia: comparison of substrate specificity for C2-modified coelenterazines. Protein Expr Purif. 2013.03; 88 (1): 150-156. ( PubMed , DOI )

  8. Tetsuo Narumi, Haruo Aikawa, Tomohiro Tanaka, Chie Hashimoto, Nami Ohashi, Wataru Nomura, Takuya Kobayakawa, Hikaru Takano, Yuki Hirota, Tsutomu Murakami, Naoki Yamamoto, Hirokazu Tamamura: Low-molecular-weight CXCR4 ligands with variable spacers. ChemMedChem. 2013.01; 8 (1): 118-124. ( PubMed , DOI )

  9. Nami Ohashi, Wataru Nomura, Tetsuo Narumi & Hirokazu Tamamura: Peptide-based Ligand Screening and Functional Analysis of Protein Kinase C Biopolymers. 2013; 100 (6): 613-620.

  10. Yoshida S, Hosoya T: Synthesis of diverse aromatic oxophosphorus compounds by the Michaelis-Arbuzov-type reaction of arynes. Chem Lett. 2013; 42 (6): 583-585. ( DOI )

  11. Koyama H, Zhang Z, Ijuin R, Siqin, Son J, Hatta Y, Ohta M, Wakao M, Hosoya T, Doi H, Suzuki M.: Pd(0)-mediated rapid coupling of methyl iodide with excess amounts of benzyl- and cinnamylboronic acid esters: efficient method for incorporation of positron-emitting (11)C radionuclide into organic frameworks by coupling between two sp(3)-hybridized carbons. RSC Adv. 2013; 3 (24): 9391-9401. ( DOI )

  12. Tetsuo Narumi, Haruo Aikawa, Tomohiro Tanaka, Chie Hashimoto, Nami Ohashi, Wataru Nomura, Takuya Kobayakawa, Hikaru Takano, Yuki Hirota, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura: Low Molecular Weight CXCR4 Ligands with Variable Spacers. ChemMedChem,. 2013; 8 (1): 118-124.

  13. Tetsuo Narumi, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Yuki Hirota, Nami Ohashi, Chie Hashimoto, Wataru Nomura, Shuzo Matsushita & Hirokazu Tamamura: CD4 Mimics as HIV Entry Inhibitors: Lead Optimization Studies of the Aromatic Substituents. Bioorg. Med. Chem.,. 2013; 21 (9): 2518-2526.

  14. Wataru Nomura, Chie Hashimoto, Takaharu Suzuki, Nami Ohashi, Masayuki Fujino, Tsutomu Murakami, Naoki Yamamoto & Hirokazu Tamamura: Multimerized CHR-derived Peptides as HIV-1 Fusion Inhibitors. Bioorg. Med. Chem.,. 2013; 21 (15): 4452-4458.

  15. Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Hiroshi Tsutsumi, Masaki Haseyama, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura: Anti-HIV-1 Peptide Derivatives Based on the HIV-1 Co-receptor CXCR4. ChemMedChem,. 2013; 8 (10): 1668-1672.

  16. Wataru Nomura, Haruo Aikawa, Nami Ohashi, Emiko Urano, Mathieu Metifiot, Masayuki Fujino, Kasthuraiah Maddali, Taro Ozaki, Ami Nozue, Tetsuo Narumi, Chie Hashimoto, Tomohiro Tanaka, Yves Pommier, Naoki Yamamoto, Jun Komano, Tsutomu Murakami & Hirokazu Tamamura: Cell-Permeable Stapled Peptides Based on HIV-1 Integrase Inhibitors Derived from HIV-1 Gene Product. ACS Chem. Biol.,. 2013; 8 (10): 2235-2244.

  17. Hiroyuki Otsuki, Takayuki Hishiki, Tomoyuki Miura, Chie Hashimoto, Tetsuo Narumi, Hirokazu Tamamura, Kazuhisa Yoshimura, Shuzo Matsushita & Tatsuhiko Igarashi: Generation of a Replication-competent Simian–human Immunodeficiency Virus, the Neutralisation Sensitivity of Which can be Enhanced in the Presence of a Small Molecule CD4 Mimic. J. Gen. Virol.,. 2013; 94 (12): 2710-2716.

  18. Chie Hashimoto, Wataru Nomura, Tetsuo Narumi, Masayuki Fujino, Toru Nakahara, Naoki Yamamoto, Tsutomu Murakami & Hirokazu Tamamura: CXCR4-derived Synthetic Peptides Inducing Anti-HIV-1 Antibodies. Bioorg. Med. Chem.,. 2013; 21 (22): 6878-6885.

  19. Chie Hashimoto, Tetsuo Narumi, Hiroyuki Otsuki, Yuki Hirota, Hiroshi Arai, Kazuhisa Yoshimura, Shigeyoshi Harada, Nami Ohashi, Wataru Nomura, Tomoyuki Miura, Tatsuhiko Igarashi, Shuzo Matsushita & Hirokazu Tamamura: A CD4 Mimic as an HIV Entry Inhibitor: Pharmacokinetics. Bioorg. Med. Chem.,. 2013; 21 (24): 7884-7889.

  1. Tetsuo Narumi, Takuya Kobayakawa, Haruo Aikawa, Shunsuke Seike, Hirokazu Tamamura: Stereoselective formation of trisubstituted (Z)-chloroalkenes adjacent to a tertiary carbon stereogenic center by organocuprate-mediated reduction/alkylation. Organic Letters. 2012.09; 14 (17): 4490-4493. ( PubMed , DOI )

  2. Ken Sakamoto, Kohei Sato, Akira Shigenaga, Kohei Tsuji, Shugo Tsuda, Hajime Hibino, Yuji Nishiuchi, Akira Otaka: Synthetic procedure for N-Fmoc amino acyl-N-sulfanylethylaniline linker as crypto-peptide thioester precursor with application to native chemical ligation. J. Org. Chem.. 2012.08; 77 (16): 6948-6958. ( PubMed , DOI )

  3. Yoshimura SH, Khan S, Ohno S, Yokogawa T, Nishikawa K, Hosoya T, Maruyama H, Nakayama Y, Takeyasu K: Site-specific attachment of a protein to a carbon nanotube end without loss of protein function. Bioconjug Chem. 2012.07; 23 (7): 1488-1493. ( PubMed , DOI )

  4. Narumi T, Tanaka T, Hashimoto C, Nomura W, Aikawa H, Sohma A, Itotani K, Kawamata M, Murakami T, Yamamoto N, Tamamura H: Pharmacophore-based small molecule CXCR4 ligands. Bioorg Med Chem Lett. 2012.06; 22 (12): 4169-4172. ( PubMed , DOI )

  5. Hashimoto C, Nomura W, Ohya A, Urano E, Miyauchi K, Narumi T, Aikawa H, Komano JA, Yamamoto N, Tamamura H: Evaluation of a synthetic C34 trimer of HIV-1 gp41 as AIDS vaccines. Bioorg Med Chem. 2012.05; 20 (10): 3287-3291. ( PubMed , DOI )

  6. Sumida Y, Kato T, Yoshida S, Hosoya T: Palladium-catalyzed regio- and stereoselective hydrosilylation of electron-deficient alkynes. Org Lett. 2012.03; 14 (6): 1552-1555. ( PubMed , DOI )

  7. Narumi T, Komoriya M, Hashimoto C, Wu H, Nomura W, Suzuki S, Tanaka T, Chiba J, Yamamoto N, Murakami T, Tamamura H: Conjugation of cell-penetrating peptides leads to identification of anti-HIV peptides from matrix proteins. Bioorg Med Chem. 2012.02; 20 (4): 1468-1474. ( PubMed , DOI )

  8. Nomura W, Hashimoto C, Ohya A, Miyauchi K, Urano E, Tanaka T, Narumi T, Nakahara T, Komano JA, Yamamoto N, Tamamura H: A synthetic C34 trimer of HIV-1 gp41 shows significant increase in inhibition potency. ChemMedChem. 2012.02; 7 (2): 205-208. ( PubMed , DOI )

  9. Nomura W, Masuda A, Ohba K, Urabe A, Ito N, Ryo A, Yamamoto N, Tamamura H: Effects of DNA binding of the zinc finger and linkers for domain fusion on the catalytic activity of sequence-specific chimeric recombinases determined by a facile fluorescent system. Biochemistry. 2012.02; 51 (7): 1510-1517. ( PubMed , DOI )

  10. Tetsuo Narumi, Takuya Kobayakawa, Haruo Aikawa, Shunsuke Seike & Hirokazu Tamamura: Stereoselective Formation of Trisubstituted (Z)-Chloroalkenes Adjacent to a Tertiary Carbon Stereogenic Center by Organocuprate-Mediated Reduction/Alkylation. Org. Lett., 14(17), 4490-4493. 2012; 14 (17): 4490-4493.

  1. Ozawa M, Takahashi K, Akazawa KH, Takashima T, Nagata H, Doi H, Hosoya T, Wada Y, Cui Y, Kataoka Y, Watanabe Y: PET of aromatase in gastric parietal cells using 11C-vorozole. J Nucl Med. 2011.12; 52 (12): 1964-1969. ( PubMed , DOI )

  2. Narumi T, Arai H, Yoshimura K, Harada S, Nomura W, Matsushita S, Tamamura H: Small molecular CD4 mimics as HIV entry inhibitors. Bioorg Med Chem. 2011.11; 19 (22): 6735-6742. ( PubMed , DOI )

  3. Hashimoto C, Tanaka T, Narumi T, Nomura W, Tamamura H: The successes and failures of HIV drug discovery. Expert Opin Drug Discov. 2011.10; 6 (10): 1067-1090. ( PubMed , DOI )

  4. Kohei Sato, Akira Shigenaga, Kohei Tsuji, Shugo Tsuda, Yoshitake Sumikawa, Ken Sakamoto, Akira Otaka: N-sulfanylethylanilide peptide as a crypto-thioester peptide. Chembiochem. 2011.08; 12 (12): 1840-1844. ( PubMed , DOI )

  5. Kohei Tsuji, Akira Shigenaga, Yoshitake Sumikawa, Kosuke Tanegashima, Kohei Sato, Keisuke Aihara, Takahiko Hara, Akira Otaka: Application of N-C- or C-N-directed sequential native chemical ligation to the preparation of CXCL14 analogs and their biological evaluation. Bioorg. Med. Chem.. 2011.07; 19 (13): 4014-4020. ( PubMed , DOI )

  6. Yamada M, Kubo H, Kobayashi S, Ishizawa K, He M, Suzuki T, Fujino N, Kunishima H, Hatta M, Nishimaki K, Aoyagi T, Tokuda K, Kitagawa M, Yano H, Tamamura H, Fujii N, Kaku M: The increase in surface CXCR4 expression on lung extravascular neutrophils and its effects on neutrophils during endotoxin-induced lung injury. Cell Mol Immunol. 2011.07; 8 (4): 305-314. ( PubMed , DOI )

  7. Xu C, Liu J, Chen L, Liang S, Fujii N, Tamamura H, Xiong H: HIV-1 gp120 enhances outward potassium current via CXCR4 and cAMP-dependent protein kinase A signaling in cultured rat microglia. Glia. 2011.06; 59 (6): 997-1007. ( PubMed , DOI )

  8. Takahashi K, Onoe K, Doi H, Nagata H, Yamagishi G, Hosoya T, Tamura Y, Wada Y, Yamanaka H, Yokoyama C, Mizuma H, Takashima T, Bergström M, Onoe H, Långström B, Watanabe Y: Increase in hypothalamic aromatase in macaque monkeys treated with anabolic-androgenic steroids: PET study with [11C]vorozole. NeuroReport. 2011.05; 22 (7): 326-330. ( PubMed , DOI )

  9. Nomura W, Ohashi N, Okuda Y, Narumi T, Ikura T, Ito N, Tamamura H: Fluorescence-quenching screening of protein kinase C ligands with an environmentally sensitive fluorophore. Bioconjug Chem. 2011.05; 22 (5): 923-930. ( PubMed , DOI )

  10. Tanaka T, Narumi T, Ozaki T, Sohma A, Ohashi N, Hashimoto C, Itotani K, Nomura W, Murakami T, Yamamoto N, Tamamura H: Azamacrocyclic metal complexes as CXCR4 antagonists. ChemMedChem. 2011.05; 6 (5): 834-839. ( PubMed , DOI )

  11. Nomura W, Narumi T, Ohashi N, Serizawa Y, Lewin NE, Blumberg PM, Furuta T, Tamamura H: Synthetic caged DAG-lactones for photochemically controlled activation of protein kinase C. Chembiochem. 2011.03; 12 (4): 535-539. ( PubMed , DOI )

  12. Tsutsumi H, Abe S, Mino T, Nomura W, Tamamura H: Intense blue fluorescence in a leucine zipper assembly. Chembiochem. 2011.03; 12 (5): 691-694. ( PubMed , DOI )

  13. Takahashi K, Yamagishi G, Hiramatsu T, Hosoya A, Onoe K, Doi H, Nagata H, Wada Y, Onoe H, Watanabe Y, Hosoya T: Practical synthesis of precursor of [N-methyl-11C]vorozole, an efficient PET tracer targeting aromatase in the brain. Bioorg Med Chem. 2011.02; 19 (4): 1464-1470. ( PubMed , DOI )

  14. Ohashi N, Nomura W, Narumi T, Lewin NE, Itotani K, Blumberg PM, Tamamura H: Fluorescent-responsive synthetic C1b domains of protein kinase Cdelta as reporters of specific high-affinity ligand binding. Bioconjug Chem. 2011.01; 22 (1): 82-87. ( PubMed , DOI )

  15. Yoshida S, Shiraishi A, Kanno K, Matsushita T, Johmoto K, Uekusa H, Hosoya T: Enhanced clickability of doubly sterically-hindered aryl azides. Sci Rep. 2011; 1 82. ( PubMed , DOI )

  16. Anwar A, Hosoya T, Leong KM, Onogi H, Okuno Y, Hiramatsu T, Koyama H, Suzuki M, Hagiwara M, Garcia-Blanco MA: The kinase inhibitor SFV785 dislocates dengue virus envelope protein from the replication complex and blocks virus assembly. PLoS ONE. 2011; 6 (8): e23246. ( PubMed , DOI )

  17. Islam MS, Nagasaka R, Ohara K, Hosoya T, Ozaki H, Ushio H, Hori M: Biological abilities of rice bran-derived antioxidant phytochemicals for medical therapy. Curr Top Med Chem. 2011; 11 (14): 1847-1853. ( PubMed )

  18. Sakai D, Kii I, Nakagawa K, Matsumoto HN, Takahashi M, Yoshida S, Hosoya T, Takakuda K, Kudo A: Remodeling of actin cytoskeleton in mouse periosteal cells under mechanical loading induces periosteal cell proliferation during bone formation. PLoS ONE. 2011; 6 (9): e24847. ( PubMed , DOI )

  1. Inouye S, Iimori R, Sahara Y, Hisada S, Hosoya T: Application of new semisynthetic aequorins with long half-decay time of luminescence to G-protein-coupled receptor assay. Anal Biochem. 2010.12; 407 (2): 247-252. ( PubMed , DOI )

  2. Abe Y, Okumura E, Hosoya T, Hirota T, Kishimoto T: A single starfish Aurora kinase performs the combined functions of Aurora-A and Aurora-B in human cells. J Cell Sci. 2010.11; 123 (Pt 22): 3978-3988. ( PubMed , DOI )

  3. Tanaka T, Nomura W, Narumi T, Masuda A, Tamamura H: Bivalent ligands of CXCR4 with rigid linkers for elucidation of the dimerization state in cells. J Am Chem Soc. 2010.11; 132 (45): 15899-15901. ( PubMed , DOI )

  4. Ogawa Y., Nonaka Y., Goto T., Ohnishi E., Hiramatsu T., Kii I., Yoshida M., Ikura T., Onogi H., Shibuya H., Hosoya T., Ito N., Hagiwara M.: Development of a novel selective inhibitor of the Downsyndrome-related kinase Dyrk1A. Nat. Commun.. 2010.10; ( PubMed , DOI )

  5. Kohta R, Kotake Y, Hosoya T, Hiramatsu T, Otsubo Y, Koyama H, Hirokane Y, Yokoyama Y, Ikeshoji H, Oofusa K, Suzuki M, Ohta S: 1-Benzyl-1,2,3,4-tetrahydroisoquinoline binds with tubulin beta, a substrate of parkin, and reduces its polyubiquitination. J Neurochem. 2010.09; 114 (5): 1291-1301. ( PubMed , DOI )

  6. Kii I, Shiraishi A, Hiramatsu T, Matsushita T, Uekusa H, Yoshida S, Yamamoto M, Kudo A, Hagiwara M, Hosoya T: Strain-promoted double-click reaction for chemical modification of azido-biomolecules. Org Biomol Chem. 2010.09; 8 (18): 4051-4055. ( PubMed , DOI )

  7. Yoshimura K, Harada S, Shibata J, Hatada M, Yamada Y, Ochiai C, Tamamura H, Matsushita S: Enhanced exposure of human immunodeficiency virus type 1 primary isolate neutralization epitopes through binding of CD4 mimetic compounds. J Virol. 2010.08; 84 (15): 7558-7568. ( PubMed , DOI )

  8. Suzuki S, Urano E, Hashimoto C, Tsutsumi H, Nakahara T, Tanaka T, Nakanishi Y, Maddali K, Han Y, Hamatake M, Miyauchi K, Pommier Y, Beutler JA, Sugiura W, Fuji H, Hoshino T, Itotani K, Nomura W, Narumi T, Yamamoto N, Komano JA, Tamamura H: Peptide HIV-1 Integrase Inhibitors from HIV-1 Gene Products. J Med Chem. 2010.07; 53 (14): 5356-5360. ( PubMed , DOI )

  9. Suzuki S, Maddali K, Hashimoto C, Urano E, Ohashi N, Tanaka T, Ozaki T, Arai H, Tsutsumi H, Narumi T, Nomura W, Yamamoto N, Pommier Y, Komano JA, Tamamura H: Peptidic HIV integrase inhibitors derived from HIV gene products: Structure-activity relationship studies. Bioorg Med Chem. 2010.07; 18 6771-6775. ( PubMed , DOI )

  10. Melchionna R, Di Carlo A, De Mori R, Cappuzzello C, Barberi L, Musaro A, Cencioni C, Fujii N, Tamamura H, Crescenzi M, Capogrossi MC, Napolitano M, Germani A: Induction of myogenic differentiation by SDF-1 via CXCR4 and CXCR7 receptors. Muscle Nerve. 2010.06; 41 (6): 828-835. ( PubMed , DOI )

  11. Nakahara T, Nomura W, Ohba K, Ohya A, Tanaka T, Hashimoto C, Narumi T, Murakami T, Yamamoto N, Tamamura H: Remodeling of dynamic structures of HIV-1 envelope proteins leads to synthetic antigen molecules inducing neutralizing antibodies. Bioconjug Chem. 2010.04; 21 (4): 709-714. ( PubMed , DOI )

  12. Aoki T, Shimizu S, Urano E, Futahashi Y, Hamatake M, Tamamura H, Terashima K, Murakami T, Yamamoto N, Komano J: Improvement of lentiviral vector-mediated gene transduction by genetic engineering of the structural protein Pr55(Gag). Gene Ther. 2010.04; 17 (9): 1124-1133. ( PubMed , DOI )

  13. Yamada Y, Ochiai C, Yoshimura K, Tanaka T, Ohashi N, Narumi T, Nomura W, Harada S, Matsushita S, Tamamura H: CD4 mimics targeting the mechanism of HIV entry. Bioorg Med Chem Lett. 2010.01; 20 (1): 354-358. ( PubMed , DOI )

  14. Narumi T, Ochiai C, Yoshimura K, Harada S, Tanaka T, Nomura W, Arai H, Ozaki T, Ohashi N, Matsushita S, Tamamura H: CD4 mimics targeting the HIV entry mechanism and their hybrid molecules with a CXCR4 antagonist. Bioorg Med Chem Lett. 2010; 20 5853-5858. ( PubMed , DOI )

  15. Nomura W, Mino T, Narumi T, Ohashi N, Masuda A, Hashimoto C, Tsutsumi H, Tamamura H: Development of crosslink-type tag-probe pairs for fluorescent imaging of proteins. Biopolymers. 2010; 94 843-852. ( PubMed , DOI )

  1. Islam MS, Yoshida H, Matsuki N, Ono K, Nagasaka R, Ushio H, Guo Y, Hiramatsu T, Hosoya T, Murata T, Hori M, Ozaki H: Antioxidant, free radical-scavenging, and NF-kappaB-inhibitory activities of phytosteryl ferulates: structure-activity studies. J Pharmacol Sci. 2009.12; 111 (4): 328-337. ( PubMed )

  2. Ikemoto T, Hosoya T, Takata K, Aoyama H, Hiramatsu T, Onoe H, Suzuki M, Endo M: Functional role of neuroendocrine-specific protein-like 1 in membrane translocation of GLUT4. Diabetes. 2009.12; 58 (12): 2802-2812. ( PubMed , DOI )

  3. Suzuki M, Sumi K, Koyama H, Siqin, Hosoya T, Takashima-Hirano M, Doi H: Pd(0)-Mediated rapid coupling between methyl iodide and heteroarylstannanes: an efficient and general method for the incorporation of a positron-emitting (11)C radionuclide into heteroaromatic frameworks. Chem Eur J. 2009.11; 15 (45): 12489-12495. ( PubMed , DOI )

  4. Ohashi N, Nomura W, Kato M, Narumi T, Lewin NE, Blumberg PM, Tamamura H: Synthesis of protein kinase Cdelta C1b domain by native chemical ligation methodology and characterization of its folding and ligand binding. J Pept Sci. 2009.10; 15 (10): 642-646. ( PubMed , DOI )

  5. Tanaka T, Nomura W, Narumi T, Esaka A, Oishi S, Ohashi N, Itotani K, Evans BJ, Wang ZX, Peiper SC, Fujii N, Tamamura H: Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids. Org Biomol Chem. 2009.09; 7 (18): 3805-3809. ( PubMed , DOI )

  6. Inouye S, Hosoya T: Reconstitution of blue fluorescent protein from recombinant apoaequorin and synthetic coelenteramide. Biochem Biophys Res Commun. 2009.09; 386 (4): 617-622. ( PubMed , DOI )

  7. Hosoya T, Inoue A, Hiramatsu T, Aoyama H, Ikemoto T, Suzuki M: Facile synthesis of diazido-functionalized biaryl compounds as radioisotope-free photoaffinity probes by Suzuki-Miyaura coupling. Bioorg Med Chem. 2009.03; 17 (6): 2490-2496. ( PubMed , DOI )

  8. Kuramori C, Azuma M, Kume K, Kaneko Y, Inoue A, Yamaguchi Y, Kabe Y, Hosoya T, Kizaki M, Suematsu M, Handa H: Capsaicin binds to prohibitin 2 and displaces it from the mitochondria to the nucleus. Biochem Biophys Res Commun. 2009.02; 379 (2): 519-525. ( PubMed , DOI )

  9. Inaba Y, Yoshimoto N, Sakamaki Y, Nakabayashi M, Ikura T, Tamamura H, Ito N, Shimizu M, Yamamoto K: A New Class of Vitamin D Analogues that Induce Structural Rearrangement of the Ligand-Binding Pocket of the Receptor. J Med Chem. 2009.02; ( PubMed , DOI )

  10. Mizukoshi F, Baba K, Goto-Koshino Y, Setoguchi-Mukai A, Fujino Y, Ohno K, Tamamura H, Oishi S, Fujii N, Tsujimoto H: Inhibitory effect of newly developed CXC-chemokine receptor 4 antagonists on the infection with feline immunodeficiency virus. J Vet Med Sci. 2009.01; 71 (1): 121-124. ( PubMed )

  11. Tsutsumi H, Nomura W, Abe S, Mino T, Masuda A, Ohashi N, Tanaka T, Ohba K, Yamamoto N, Akiyoshi K, Tamamura H: Fluorogenically active leucine zipper peptides as tag-probe pairs for protein imaging in living cells. Angew Chem Int Ed Engl. 2009; 48 (48): 9164-9166. ( PubMed , DOI )

  12. Doi H, Ban I, Nonoyama A, Sumi K, Kuang C, Hosoya T, Tsukada H, Suzuki M: Palladium(0)-mediated rapid methylation and fluoromethylation on carbon frameworks by reacting methyl and fluoromethyl iodide with aryl and alkenyl boronic acid esters: useful for the synthesis of [11C]CH(3)--C- and [18F]FCH2--C-Containing PET tracers (PET=positron emission tomography). Chem Eur J. 2009; 15 (16): 4165-4171. ( PubMed , DOI )

  13. Tamamura H, Tanaka T, Tsutsumi H, Ohashi N, Hiramatsu K, Araki T, Ojida A, Hamachi I, Wang Z, Peiper SC, Trent JO, Ueda S, Oishi S, Fujii N: Development of chemokine receptor CXCR4 antagonists using bio-mimetic strategy. Adv Exp Med Biol. 2009; 611 145-146. ( PubMed )

  14. Tamamura H, Tanaka T, Tsutsumi H, Nemoto K, Mizokami S, Ohashi N, Oishi S, Fujii N: Stereoselective synthesis of peptidomimetics based on acid-catalyzed ring-opening of beta-aziridinyl-alpha,beta-enoates. Adv Exp Med Biol. 2009; 611 149-150. ( PubMed )

  1. Tanaka T, Tsutsumi H, Nomura W, Tanabe Y, Ohashi N, Esaka A, Ochiai C, Sato J, Itotani K, Murakami T, Ohba K, Yamamoto N, Fujii N, Tamamura H: Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore. Org Biomol Chem. 2008.12; 6 (23): 4374-4377. ( PubMed , DOI )

  2. Nomura W, Tanabe Y, Tsutsumi H, Tanaka T, Ohba K, Yamamoto N, Tamamura H: Fluorophore labeling enables imaging and evaluation of specific CXCR4-ligand interaction at the cell membrane for fluorescence-based screening. Bioconjug Chem. 2008.09; 19 (9): 1917-1920. ( PubMed , DOI )

  3. Nakata H, Steinberg SM, Koh Y, Maeda K, Takaoka Y, Tamamura H, Fujii N, Mitsuya H: Potent synergistic anti-human immunodeficiency virus (HIV) effects using combinations of the CCR5 inhibitor aplaviroc with other anti-HIV drugs. Antimicrob Agents Chemother. 2008.06; 52 (6): 2111-2119. ( PubMed , DOI )

  4. Driessen WH, Fujii N, Tamamura H, Sullivan SM: Development of peptide-targeted lipoplexes to CXCR4-expressing rat glioma cells and rat proliferating endothelial cells. Mol Ther. 2008.03; 16 (3): 516-524. ( PubMed , DOI )

  5. Yomoda J, Muraki M, Kataoka N, Hosoya T, Suzuki M, Hagiwara M, Kimura H: Combination of Clk family kinase and SRp75 modulates alternative splicing of Adenovirus E1A. Genes Cells. 2008.03; 13 (3): 233-244. ( PubMed , DOI )

  6. Hirokazu Tamamura, Hiroshi Tsutsumi, Wataru Nomura, Tomohiro Tanaka & Nobutaka Fujii: A Future Perspective on the Development of Chemokine Receptor CXCR4 Antagonists. Expert Opin. Drug Discovery. 2008; 3 (10): 1150-1166.

  7. Kasiyanov A, Fujii N, Tamamura H, Xiong H: Modulation of network-driven, GABA-mediated giant depolarizing potentials by SDF-1alpha in the developing hippocampus. Dev Neurosci. 2008; 30 (4): 285-292. ( PubMed , DOI )

  8. Tamamura H, Tsutsumi H, Nomura W, Fujii N: Exploratory studies on development of the chemokine receptor CXCR4 antagonists toward downsizing. Perspect Medicin Chem. 2008; 2 1-9. ( PubMed )

  1. Kabashima K, Sugita K, Shiraishi N, Tamamura H, Fujii N, Tokura Y: CXCR4 engagement promotes dendritic cell survival and maturation. Biochem Biophys Res Commun. 2007.10; 361 (4): 1012-1016. ( PubMed , DOI )

  2. Kabashima K, Shiraishi N, Sugita K, Mori T, Onoue A, Kobayashi M, Sakabe J, Yoshiki R, Tamamura H, Fujii N, Inaba K, Tokura Y: CXCL12-CXCR4 engagement is required for migration of cutaneous dendritic cells. Am J Pathol. 2007.10; 171 (4): 1249-1257. ( PubMed , DOI )

  3. Hiramatsu T, Guo Y, Hosoya T: 3-Azidodifluoromethyl-3H-diazirin-3-yl group as an all-in-one functional group for radioisotope-free photoaffinity labeling. Org Biomol Chem. 2007.09; 5 (18): 2916-2919. ( PubMed , DOI )

  4. Abe M, Ohno S, Yokogawa T, Nakanishi T, Arisaka F, Hosoya T, Hiramatsu T, Suzuki M, Ogasawara T, Sawasaki T, Nishikawa K, Kitamura M, Hori H, Endo Y: Detection of structural changes in a cofactor binding protein by using a wheat germ cell-free protein synthesis system coupled with unnatural amino acid probing. Proteins. 2007.05; 67 (3): 643-652. ( PubMed , DOI )

  5. Kubonishi S, Kikuchi T, Yamaguchi S, Tamamura H, Fujii N, Watanabe T, Arenzana-Seisdedos F, Ikeda K, Matsui T, Tanimoto M, Katayama Y: Rapid hematopoietic progenitor mobilization by sulfated colominic acid. Biochem Biophys Res Commun. 2007.04; 355 (4): 970-975. ( PubMed , DOI )

  6. Ohno S, Matsui M, Yokogawa T, Nakamura M, Hosoya T, Hiramatsu T, Suzuki M, Hayashi N, Nishikawa K: Site-selective post-translational modification of proteins using an unnatural amino acid, 3-azidotyrosine. J Biochem. 2007.03; 141 (3): 335-343. ( PubMed , DOI )

  7. Berchiche YA, Chow KY, Lagane B, Leduc M, Percherancier Y, Fujii N, Tamamura H, Bachelerie F, Heveker N: Direct assessment of CXCR4 mutant conformations reveals complex link between receptor structure and G(alpha)(i) activation. J Biol Chem. 2007.02; 282 (8): 5111-5115. ( PubMed , DOI )

  8. Ueda S, Oishi S, Wang ZX, Araki T, Tamamura H, Cluzeau J, Ohno H, Kusano S, Nakashima H, Trent JO, Peiper SC, Fujii N: Structure-activity relationships of cyclic peptide-based chemokine receptor CXCR4 antagonists: disclosing the importance of side-chain and backbone functionalities. J Med Chem. 2007.01; 50 (2): 192-198. ( PubMed , DOI )

  9. Tsutsumi H, Tanaka T, Ohashi N, Masuno H, Tamamura H, Hiramatsu K, Araki T, Ueda S, Oishi S, Fujii N: Therapeutic potential of the chemokine receptor CXCR4 antagonists as multifunctional agents. Biopolymers. 2007; 88 (2): 279-289. ( PubMed , DOI )

  10. Tamamura H, Tsutsumi H, Masuno H, Fujii N: Development of low molecular weight CXCR4 antagonists by exploratory structural tuning of cyclic tetra- and pentapeptide-scaffolds towards the treatment of HIV infection, cancer metastasis and rheumatoid arthritis. Curr Med Chem. 2007; 14 (1): 93-102. ( PubMed )

  11. Hiroshi Tsutsumi, Hirokazu Tamamura & Nobutaka Fujii: Inhibitors of the Chemokine Receptor CXCR4. Chemotherapy of AIDS, Metastatic Cancer, Leukemia and Rheumatoid Arthritis. Lett. Drug Design Discovery. 2007; 4 20-26.

  12. Hirokazu Tamamura, Tomohiro Tanaka, Hiroshi Tsutsumi, Koji Nemoto, Satoko Mizokami, Nami Ohashi, Shinya Oishi & Nobutaka Fujii: Versatile Use of Acid-catalyzed Ring-opening of β-Aziridinyl-α,β-enoates to Stereoselective Synthesis of Peptidomimetics. Tetrahedron. 2007; 63 9243-9254.

  1. Cui Y, Takamatsu H, Kakiuchi T, Ohba H, Kataoka Y, Yokoyama C, Onoe H, Watanabe Y, Hosoya T, Suzuki M, Noyori R, Tsukada H, Watanabe Y: Neuroprotection by a central nervous system-type prostacyclin receptor ligand demonstrated in monkeys subjected to middle cerebral artery occlusion and reperfusion: a positron emission tomography study. Stroke. 2006.11; 37 (11): 2830-2836. ( PubMed , DOI )

  2. Tamamura H, Tsutsumi H, Fujii N: The chemokine receptor CXCR4 as a therapeutic target for several diseases. Mini Rev Med Chem. 2006.09; 6 (9): 989-995. ( PubMed )

  3. MEDI 150-Design and synthesis of histone deacetylase 6 selective inhibitors 2006.09; 232

  4. Suzuki Takayoshi, Kouketsu Akiyasu, Itoh Yukihiro, Hisakawa Shinya, Nakagawa Hidehiko, Miyata Naoki: P-440 DISCOVERY OF NOVEL HISTONE DEACETYLASE 6 SELECTIVE INHIBITORS International Symposium on the Chemistry of Natural Products. 2006.07; 2006 "P-440". ( DOI )

  5. Fukuhara T, Hosoya T, Shimizu S, Sumi K, Oshiro T, Yoshinaka Y, Suzuki M, Yamamoto N, Herzenberg LA, Herzenberg LA, Hagiwara M: Utilization of host SR protein kinases and RNA-splicing machinery during viral replication. Proc Natl Acad Sci USA. 2006.07; 103 (30): 11329-11333. ( PubMed , DOI )

  6. Tamamura H, Tsutsumi H, Masuno H, Mizokami S, Hiramatsu K, Wang Z, Trent JO, Nakashima H, Yamamoto N, Peiper SC, Fujii N: Development of a linear type of low molecular weight CXCR4 antagonists based on T140 analogs. Org Biomol Chem. 2006.06; 4 (12): 2354-2357. ( PubMed , DOI )

  7. Tamamura H, Ojida A, Ogawa T, Tsutsumi H, Masuno H, Nakashima H, Yamamoto N, Hamachi I, Fujii N: Identification of a new class of low molecular weight antagonists against the chemokine receptor CXCR4 having the dipicolylamine-zinc(II) complex structure. J Med Chem. 2006.06; 49 (11): 3412-3415. ( PubMed , DOI )

  8. Menu E, Asosingh K, Indraccolo S, De Raeve H, Van Riet I, Van Valckenborgh E, Vande Broek I, Fujii N, Tamamura H, Van Camp B, Vanderkerken K: The involvement of stromal derived factor 1alpha in homing and progression of multiple myeloma in the 5TMM model. Haematologica. 2006.05; 91 (5): 605-612. ( PubMed )

  9. Hanaoka H, Mukai T, Tamamura H, Mori T, Ishino S, Ogawa K, Iida Y, Doi R, Fujii N, Saji H: Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors. Nucl Med Biol. 2006.05; 33 (4): 489-494. ( PubMed , DOI )

  10. Niida A, Tanigaki H, Inokuchi E, Sasaki Y, Oishi S, Ohno H, Tamamura H, Wang Z, Peiper SC, Kitaura K, Otaka A, Fujii N: Stereoselective synthesis of 3,6-disubstituted-3,6-dihydropyridin-2-ones as potential diketopiperazine mimetics using organocopper-mediated anti-SN2' reactions and their use in the preparation of low-molecule CXCR4 antagonists. J Org Chem. 2006.05; 71 (10): 3942-3951. ( PubMed , DOI )

  11. Kasyanov A, Tamamura H, Fujii N, Xiong H: HIV-1 gp120 enhances giant depolarizing potentials via chemokine receptor CXCR4 in neonatal rat hippocampus. Eur J Neurosci. 2006.03; 23 (5): 1120-1128. ( PubMed , DOI )

  12. Hosoya T, Sumi K, Doi H, Wakao M, Suzuki M: Rapid methylation on carbon frameworks useful for the synthesis of 11CH3-incorporated PET tracers: Pd(0)-mediated rapid coupling of methyl iodide with an alkenyltributylstannane leading to a 1-methylalkene. Org Biomol Chem. 2006.02; 4 (3): 410-415. ( PubMed , DOI )

  13. Tamamura H, Tsutsumi H: Specific probes for chemokine receptors. Chem Biol. 2006.01; 13 (1): 8-10. ( PubMed , DOI )

  14. Niida A, Wang Z, Tomita K, Oishi S, Tamamura H, Otaka A, Navenot JM, Broach JR, Peiper SC, Fujii N: Design and synthesis of downsized metastin (45-54) analogs with maintenance of high GPR54 agonistic activity. Bioorg Med Chem Lett. 2006.01; 16 (1): 134-137. ( PubMed , DOI )

  15. Shinya Oishi, Kazuhide Miyamoto, Ayumu Niida, Mikio Yamamoto, Keiichi Ajito, Hirokazu Tamamura, Akira Otaka, Yoshihiro Kuroda, Akira Asai & Nobutaka Fujii: Application of Tri- and Tetrasubstituted Alkene Dipeptide Mimetics to Conformational Studies of Cyclic RGD Peptides. Tetrahedron. 2006; 62 1416-1424.

  16. Hirokazu Tamamura & Hiroshi Tsutsumi: Specific Probes for Chemokine Receptors Chem. Biol.. 2006; 13 8-10.

  1. Tamamura H, Esaka A, Ogawa T, Araki T, Ueda S, Wang Z, Trent JO, Tsutsumi H, Masuno H, Nakashima H, Yamamoto N, Peiper SC, Otaka A, Fujii N: Structure-activity relationship studies on CXCR4 antagonists having cyclic pentapeptide scaffolds. Org Biomol Chem. 2005.12; 3 (24): 4392-4394. ( PubMed , DOI )

  2. Tamamura H, Fujii N: The therapeutic potential of CXCR4 antagonists in the treatment of HIV infection, cancer metastasis and rheumatoid arthritis. Expert Opin Ther Targets. 2005.12; 9 (6): 1267-1282. ( PubMed , DOI )

  3. Ueda S, Fujita M, Tamamura H, Fujii N, Otaka A: Photolabile protection for one-pot sequential native chemical ligation. Chembiochem. 2005.11; 6 (11): 1983-1986. ( PubMed , DOI )

  4. Tamamura H, Otaka A, Fujii N: Development of anti-HIV agents targeting dynamic supramolecular mechanism: entry and fusion inhibitors based on CXCR4/CCR5 antagonists and gp41-C34-remodeling peptides. Curr HIV Res. 2005.10; 3 (4): 289-301. ( PubMed )

  5. Burger M, Hartmann T, Krome M, Rawluk J, Tamamura H, Fujii N, Kipps TJ, Burger JA: Small peptide inhibitors of the CXCR4 chemokine receptor (CD184) antagonize the activation, migration, and antiapoptotic responses of CXCL12 in chronic lymphocytic leukemia B cells. Blood. 2005.09; 106 (5): 1824-1830. ( PubMed , DOI )

  6. Tamamura H, Araki T, Ueda S, Wang Z, Oishi S, Esaka A, Trent JO, Nakashima H, Yamamoto N, Peiper SC, Otaka A, Fujii N: Identification of novel low molecular weight CXCR4 antagonists by structural tuning of cyclic tetrapeptide scaffolds. J Med Chem. 2005.05; 48 (9): 3280-3289. ( PubMed , DOI )

  7. Percherancier Y, Berchiche YA, Slight I, Volkmer-Engert R, Tamamura H, Fujii N, Bouvier M, Heveker N: Bioluminescence resonance energy transfer reveals ligand-induced conformational changes in CXCR4 homo- and heterodimers. J Biol Chem. 2005.03; 280 (11): 9895-9903. ( PubMed , DOI )

  8. Zannettino AC, Farrugia AN, Kortesidis A, Manavis J, To LB, Martin SK, Diamond P, Tamamura H, Lapidot T, Fujii N, Gronthos S: Elevated serum levels of stromal-derived factor-1alpha are associated with increased osteoclast activity and osteolytic bone disease in multiple myeloma patients. Cancer Res. 2005.03; 65 (5): 1700-1709. ( PubMed , DOI )

  9. Hosoya T, Hiramatsu T, Ikemoto T, Aoyama H, Ohmae T, Endo M, Suzuki M: Design of dantrolene-derived probes for radioisotope-free photoaffinity labeling of proteins involved in the physiological Ca2+ release from sarcoplasmic reticulum of skeletal muscle. Bioorg Med Chem Lett. 2005.03; 15 (5): 1289-1294. ( PubMed , DOI )

  10. Piovan E, Tosello V, Indraccolo S, Cabrelle A, Baesso I, Trentin L, Zamarchi R, Tamamura H, Fujii N, Semenzato G, Chieco-Bianchi L, Amadori A: Chemokine receptor expression in EBV-associated lymphoproliferation in hu/SCID mice: implications for CXCL12/CXCR4 axis in lymphoma generation. Blood. 2005.02; 105 (3): 931-939. ( PubMed , DOI )

  11. Nameki D, Kodama E, Ikeuchi M, Mabuchi N, Otaka A, Tamamura H, Ohno M, Fujii N, Matsuoka M: Mutations conferring resistance to human immunodeficiency virus type 1 fusion inhibitors are restricted by gp41 and Rev-responsive element functions. J Virol. 2005.01; 79 (2): 764-770. ( PubMed , DOI )

  12. Tamamura H, Hiramatsu K, Ueda S, Wang Z, Kusano S, Terakubo S, Trent JO, Peiper SC, Yamamoto N, Nakashima H, Otaka A, Fujii N: Stereoselective synthesis of [L-Arg-L/D-3-(2-naphthyl)alanine]-type (E)-alkene dipeptide isosteres and its application to the synthesis and biological evaluation of pseudopeptide analogues of the CXCR4 antagonist FC131. J Med Chem. 2005.01; 48 (2): 380-391. ( PubMed , DOI )

  13. Ayumu Niida, Shinya Oishi, Yoshikazu Sasaki, Makiko Mizumoto, Hirokazu Tamamura, Nobutaka Fujii & Akira Otaka: Facile Access to (Z)-Alkene-containing Diketopiperazine Mimetics Utilizing Organocopper-mediated Anti-SN2' Reactions. Tetrahedron Lett.. 2005; 46 4183-4186.

  14. Margitta Retz, Sachdev S. Sidhu, Jan Lehmann, Hirokazu Tamamura, Nobutaka Fujii & Carol Basbaum: New HIV-Drug Inhibits in Vitro Bladder Cancer Migration and Invasion Eur. Urol.. 2005; 48 (6): 1025-1030.

  15. Jayendra B. Bhonsle, Zi-xuan Wang, Hirokazu Tamamura, Nobutaka Fujii, Stephen C. Peiper & John O. Trent: A Simple, Automated Quasi-4D-QSAR, Quasi-multi Way PLS Approach to Develop Highly Predictive QSAR Models for Highly Flexible CXCR4 Inhibitor Cyclic Peptide Ligands Using Scripted Common Molecular Modeling Tools. QSAR Comb. Sci.. 2005; 24 (5): 620-630.

  1. Allen CD, Ansel KM, Low C, Lesley R, Tamamura H, Fujii N, Cyster JG: Germinal center dark and light zone organization is mediated by CXCR4 and CXCR5. Nat Immunol. 2004.09; 5 (9): 943-952. ( PubMed , DOI )

  2. Tamamura H, Sigano DM, Lewin NE, Peach ML, Nicklaus MC, Blumberg PM, Marquez VE: Conformationally constrained analogues of diacylglycerol (DAG). 23. Hydrophobic ligand-protein interactions versus ligand-lipid interactions of DAG-lactones with protein kinase C (PK-C). J Med Chem. 2004.09; 47 (20): 4858-4864. ( PubMed , DOI )

  3. Suzuki M, Doi H, Kato K, Hosoya T, Watanabe Y, Watanabe Y: Designed molecular probes in brain research: molecular imaging of IP2 receptor in the human brain. Jpn J Neuropsychopharmacol. 2004.08; 24 (4): 221-229. ( PubMed )

  4. Otaka A, Ueda S, Tomita K, Yano Y, Tamamura H, Matsuzaki K, Fujii N: Facile synthesis of membrane-embedded peptides utilizing lipid bilayer-assisted chemical ligation. Chem Commun (Camb). 2004.08; (15): 1722-1723. ( PubMed , DOI )

  5. Tamamura H, Fujisawa M, Hiramatsu K, Mizumoto M, Nakashima H, Yamamoto N, Otaka A, Fujii N: Identification of a CXCR4 antagonist, a T140 analog, as an anti-rheumatoid arthritis agent. FEBS Lett. 2004.07; 569 (1-3): 99-104. ( PubMed , DOI )

  6. Yamamoto N, Yang R, Yoshinaka Y, Amari S, Nakano T, Cinatl J, Rabenau H, Doerr HW, Hunsmann G, Otaka A, Tamamura H, Fujii N, Yamamoto N: HIV protease inhibitor nelfinavir inhibits replication of SARS-associated coronavirus. Biochem Biophys Res Commun. 2004.06; 318 (3): 719-725. ( PubMed , DOI )

  7. Tamamura H, Fujii N: Two orthogonal approaches to overcome multi-drug resistant HIV-1s: development of protease inhibitors and entry inhibitors based on CXCR4 antagonists. Curr Drug Targets Infect Disord. 2004.06; 4 (2): 103-110. ( PubMed )

  8. Muraki M, Ohkawara B, Hosoya T, Onogi H, Koizumi J, Koizumi T, Sumi K, Yomoda J, Murray MV, Kimura H, Furuichi K, Shibuya H, Krainer AR, Suzuki M, Hagiwara M: Manipulation of alternative splicing by a newly developed inhibitor of Clks. J Biol Chem. 2004.06; 279 (23): 24246-24254. ( PubMed , DOI )

  9. Peng H, Huang Y, Rose J, Erichsen D, Herek S, Fujii N, Tamamura H, Zheng J: Stromal cell-derived factor 1-mediated CXCR4 signaling in rat and human cortical neural progenitor cells. J Neurosci Res. 2004.04; 76 (1): 35-50. ( PubMed , DOI )

  10. Tamamura H, Mizumoto M, Hiramatsu K, Kusano S, Terakubo S, Yamamoto N, Trent JO, Wang Z, Peiper SC, Nakashima H, Otaka A, Fujii N: Topochemical exploration of potent compounds using retro-enantiomer libraries of cyclic pentapeptides. Org Biomol Chem. 2004.04; 2 (8): 1255-1257. ( PubMed , DOI )

  11. Hosoya T, Hiramatsu T, Ikemoto T, Nakanishi M, Aoyama H, Hosoya A, Iwata T, Maruyama K, Endo M, Suzuki M: Novel bifunctional probe for radioisotope-free photoaffinity labeling: compact structure comprised of photospecific ligand ligation and detectable tag anchoring units. Org Biomol Chem. 2004.03; 2 (5): 637-641. ( PubMed , DOI )

  12. Otaka A, Watanabe J, Yukimasa A, Sasaki Y, Watanabe H, Kinoshita T, Oishi S, Tamamura H, Fujii N: SmI2-mediated reduction of gamma,gamma-difluoro-alpha,beta-enoates with application to the synthesis of functionalized (Z)-fluoroalkene-type dipeptide isosteres. J Org Chem. 2004.03; 69 (5): 1634-1645. ( PubMed , DOI )

  13. Hosoya T, Wakao M, Kondo Y, Doi H, Suzuki M: Rapid methylation of terminal acetylenes by the Stille coupling of methyl iodide with alkynyltributylstannanes: a general protocol potentially useful for the synthesis of short-lived 11CH3-labeled PET tracers with a 1-propynyl group. Org Biomol Chem. 2004.01; 2 (1): 24-27. ( PubMed , DOI )

  14. Mori T, Doi R, Koizumi M, Toyoda E, Ito D, Kami K, Masui T, Fujimoto K, Tamamura H, Hiramatsu K, Fujii N, Imamura M: CXCR4 antagonist inhibits stromal cell-derived factor 1-induced migration and invasion of human pancreatic cancer. Mol Cancer Ther. 2004.01; 3 (1): 29-37. ( PubMed )

  15. Tamamura H, Sigano DM, Lewin NE, Blumberg PM, Marquez VE: Conformationally constrained analogues of diacylglycerol. 20. The search for an elusive binding site on protein kinase C through relocation of the carbonyl pharmacophore along the sn-1 side chain of 1,2-diacylglycerol lactones. J Med Chem. 2004.01; 47 (3): 644-655. ( PubMed , DOI )

  16. Suzuki M, Doi H, Hosoya T, Långström B, Watanabe Y.: Rapid methylation on carbon frameworks leading to the synthesis of a PET tracer capable of imaging a novel CNS-type prostacyclin receptor in living human brain. Trends Anal Chem. 2004; 23 (8): 595-607. ( DOI )

  17. Mitsuko Takenaga, Hirokazu Tamamura, Kenichi Hiramatsu, Natsumi Nakamura, Yoko Yamaguchi, Aki Kitagawa, Shinichi Kawai, Hideki Nakashima, Nobutaka Fujii & Rie Igarashi: A Single Treatment with Microcapsules Containing a CXCR4 Antagonist Suppresses Pulmonary Metastasis of Murine Melanoma. Biochem. Biophys. Res. Commun.. 2004; 320 (1): 226-232.

  1. Trent JO, Wang ZX, Murray JL, Shao W, Tamamura H, Fujii N, Peiper SC: Lipid bilayer simulations of CXCR4 with inverse agonists and weak partial agonists. J Biol Chem. 2003.11; 278 (47): 47136-47144. ( PubMed , DOI )

  2. Tamamura H, Hiramatsu K, Mizumoto M, Ueda S, Kusano S, Terakubo S, Akamatsu M, Yamamoto N, Trent JO, Wang Z, Peiper SC, Nakashima H, Otaka A, Fujii N: Enhancement of the T140-based pharmacophores leads to the development of more potent and bio-stable CXCR4 antagonists. Org Biomol Chem. 2003.11; 1 (21): 3663-3669. ( PubMed )

  3. Tamamura H, Hiramatsu K, Kusano S, Terakubo S, Yamamoto N, Trent JO, Wang Z, Peiper SC, Nakashima H, Otaka A, Fujii N: Synthesis of potent CXCR4 inhibitors possessing low cytotoxicity and improved biostability based on T140 derivatives. Org Biomol Chem. 2003.11; 1 (21): 3656-3662. ( PubMed )

  4. Oonuma T, Morimatsu M, Nakagawa T, Uyama R, Sasaki N, Nakaichi M, Tamamura H, Fujii N, Hashimoto S, Yamamura H, Syuto B: Role of CXCR4 and SDF-1 in mammary tumor metastasis in the cat. J Vet Med Sci. 2003.10; 65 (10): 1069-1073. ( PubMed )

  5. Tamamura H, Hori A, Kanzaki N, Hiramatsu K, Mizumoto M, Nakashima H, Yamamoto N, Otaka A, Fujii N: T140 analogs as CXCR4 antagonists identified as anti-metastatic agents in the treatment of breast cancer. FEBS Lett. 2003.08; 550 (1-3): 79-83. ( PubMed )

  6. Otaka A, Yukimasa A, Watanabe J, Sasaki Y, Oishi S, Tamamura H, Fujii N: Application of samarium diiodide (SmI2)-induced reduction of gamma-acetoxy-alpha,beta-enoates with alpha-specific kinetic electrophilic trapping for the synthesis of amino acid derivatives. Chem Commun (Camb). 2003.08; (15): 1834-1835. ( PubMed )

  7. Tamamura H, Kato T, Otaka A, Fujii N: Synthesis of potent beta-secretase inhibitors containing a hydroxyethylamine dipeptide isostere and their structure-activity relationship studies. Org Biomol Chem. 2003.07; 1 (14): 2468-2473. ( PubMed )

  8. Fujii N, Oishi S, Hiramatsu K, Araki T, Ueda S, Tamamura H, Otaka A, Kusano S, Terakubo S, Nakashima H, Broach JA, Trent JO, Wang ZX, Peiper SC: Molecular-size reduction of a potent CXCR4-chemokine antagonist using orthogonal combination of conformation- and sequence-based libraries. Angew Chem Int Ed Engl. 2003.07; 42 (28): 3251-3253. ( PubMed , DOI )

  9. Yasuda T, Poole AR, Shimizu M, Nakagawa T, Julovi SM, Tamamura H, Fujii N, Nakamura T: Involvement of CD44 in induction of matrix metalloproteinases by a COOH-terminal heparin-binding fragment of fibronectin in human articular cartilage in culture. Arthritis Rheum. 2003.05; 48 (5): 1271-1280. ( PubMed , DOI )

  10. Tamamura H, Koh Y, Ueda S, Sasaki Y, Yamasaki T, Aoki M, Maeda K, Watai Y, Arikuni H, Otaka A, Mitsuya H, Fujii N: Reduction of peptide character of HIV protease inhibitors that exhibit nanomolar potency against multidrug resistant HIV-1 strains. J Med Chem. 2003.04; 46 (9): 1764-1768. ( PubMed , DOI )

  11. Hosoya T, Aoyama H, Ikemoto T, Kihara Y, Hiramatsu T, Endo M, Suzuki M: Dantrolene analogues revisited: general synthesis and specific functions capable of discriminating two kinds of Ca2+ release from sarcoplasmic reticulum of mouse skeletal muscle. Bioorg Med Chem. 2003.03; 11 (5): 663-673. ( PubMed )

  12. Fujii N, Nakashima H, Tamamura H: The therapeutic potential of CXCR4 antagonists in the treatment of HIV. Expert Opin Investig Drugs. 2003.02; 12 (2): 185-195. ( PubMed , DOI )

  1. Hosoya T, Aoyama H, Ikemoto T, Hiramatsu T, Kihara Y, Endo M, Suzuki M: [(125)I]-N-[(3-azido-5-iodo)benzyl]dantrolene and [(125)I]-N-[[3-iodo-5-(3-trifluoromethyl-3H-diazirin-3-yl)]benzyl]dantrolene: photoaffinity probes specific for the physiological Ca(2+) release from sarcoplasmic reticulum of skeletal muscle. Bioorg Med Chem Lett. 2002.11; 12 (22): 3263-3265. ( PubMed )

  2. Oishi S, Kamano T, Niida A, Odagaki Y, Hamanaka N, Yamamoto M, Ajito K, Tamamura H, Otaka A, Fujii N: Diastereoselective synthesis of new psi[(E)-CH=CMe]- and psi[(Z)-CH=CMe]-type alkene dipeptide isosteres by organocopper reagents and application to conformationally restricted cyclic RGD peptidomimetics. J Org Chem. 2002.08; 67 (17): 6162-6173. ( PubMed )

  3. Otaka A, Nakamura M, Nameki D, Kodama E, Uchiyama S, Nakamura S, Nakano H, Tamamura H, Kobayashi Y, Matsuoka M, Fujii N: Remodeling of gp41-C34 peptide leads to highly effective inhibitors of the fusion of HIV-1 with target cells. Angew Chem Int Ed Engl. 2002.08; 41 (16): 2937-2940. ( PubMed , DOI )

  4. Otaka A, Katagiri F, Kinoshita T, Odagaki Y, Oishi S, Tamamura H, Hamanaka N, Fujii N: Regio- and stereoselective synthesis of (E)-alkene trans-Xaa-Pro dipeptide mimetics utilizing organocopper-mediated anti-S(N)2' reactions. J Org Chem. 2002.08; 67 (17): 6152-6161. ( PubMed )

  5. Zhang WB, Navenot JM, Haribabu B, Tamamura H, Hiramatu K, Omagari A, Pei G, Manfredi JP, Fujii N, Broach JR, Peiper SC: A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists. J Biol Chem. 2002.07; 277 (27): 24515-24521. ( PubMed , DOI )

  6. Tamamura H, Omagari A, Hiramatsu K, Oishi S, Habashita H, Kanamoto T, Gotoh K, Yamamoto N, Nakashima H, Otaka A, Fujii N: Certification of the critical importance of L-3-(2-naphthyl)alanine at position 3 of a specific CXCR4 inhibitor, T140, leads to an exploratory performance of its downsizing study. Bioorg Med Chem. 2002.05; 10 (5): 1417-1426. ( PubMed )

  7. Ikenoya M, Hidaka H, Hosoya T, Suzuki M, Yamamoto N, Sasaki Y: Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor. J Neurochem. 2002.04; 81 (1): 9-16. ( PubMed )

  8. Oishi S, Kamano T, Niida A, Odagaki Y, Tamamura H, Otaka A, Hamanaka N, Fujii N: Diastereoselective synthesis of psi[(E)-CH=CMe]- and psi[(Z)-CH=CMe]-type dipeptide isosteres by organocopper-mediated anti-S(N)2' reaction. Org Lett. 2002.04; 4 (7): 1051-1054. ( PubMed )

  9. Oishi S, Niida A, Kamano T, Odagaki Y, Tamamura H, Otaka A, Hamanaka N, Fujii N: Diastereoselective synthesis of psi[(E)-CMe=CH]- and psi[(E)-CMe=CMe]- type dipeptide isosteres based on organocopper-mediated anti-S(N)2' reaction. Org Lett. 2002.04; 4 (7): 1055-1058. ( PubMed )

  10. Tamamura H, Hiramatsu K, Miyamoto K, Omagari A, Oishi S, Nakashima H, Yamamoto N, Kuroda Y, Nakagawa T, Otaka A, Fujii N: Synthesis and evaluation of pseudopeptide analogues of a specific CXCR4 inhibitor, T140: the insertion of an (E)-alkene dipeptide isostere into the betaII'-turn moiety. Bioorg Med Chem Lett. 2002.03; 12 (6): 923-928. ( PubMed )

  11. Takamatsu H, Tsukada H, Watanabe Y, Cui Y, Kataoka Y, Hosoya T, Suzuki M, Watanabe Y: Specific ligand for a central type prostacyclin receptor attenuates neuronal damage in a rat model of focal cerebral ischemia. Brain Res. 2002.01; 925 (2): 176-182. ( PubMed )

  12. Hirokazu Tamamura, Tadakazu Hori, Akira Otaka & Nobutaka Fujii: Efficient Stereoselective Synthesis of Peptidomimetics Containing Hydroxyethylamine Dipeptide Isosteres Utilizing the Aza-Payne Rearrangement and O, N-Acyl Transfer Reactions. J. Chem. Soc., Perkin Trans.. 2002; 1 (2002(5)): 577-580.

  13. Hamura T, Hosoya T, Yamaguchi H, Kuriyama Y, Tanabe M, Miyamoto M, Yasui Y, Matsumoto T, Suzuki K.: Facile access to versatile polyaromatic building blocks: selectively protected benzocyclobutenedione derivatives via regioselective [2 + 2] cycloaddition of α-alkoxybenzyne and ketene silyl acetal. Helv Chim Acta. 2002; 85 (11): 3589-3604. ( DOI )

  14. Shinya Oishi, Ayumu Niida, Takae Kamano, Yoshihisa Miwa, Tooru Taga, Yoshihiko Odagaki, Nobuyuki Hamanaka, Mikio Yamamoto, Keiichi Ajito, Hirokazu Tamamura, Akira Otaka & Nobutaka Fujii: Regio- and Stereoselective Ring-opening of Chiral 1,3-Oxazolidin-2-one Derivatives by Organocopper Reagents Provides Novel Access to Di-, tri- and tetra-substituted Alkene Dipeptide Isosteres. J. Chem. Soc., Perkin Trans.. 2002; 1 (2002(15)): 1786-1793.

  1. Tamamura H: [Development of selective antagonists against an HIV second receptor] Yakugaku Zasshi. 2001.11; 121 (11): 781-792. ( PubMed )

  2. Ikemoto T, Hosoya T, Aoyama H, Kihara Y, Suzuki M, Endo M: Effects of dantrolene and its derivatives on Ca(2+) release from the sarcoplasmic reticulum of mouse skeletal muscle fibres. Br J Pharmacol. 2001.10; 134 (4): 729-736. ( PubMed , DOI )

  3. Fujii N, Tamamura H: Peptide-lead CXCR4 antagonists with high anti-HIV activity. Curr Opin Investig Drugs. 2001.09; 2 (9): 1198-1202. ( PubMed )

  4. Tamamura H, Omagari A, Hiramatsu K, Kanamoto T, Gotoh K, Kanbara K, Yamamoto N, Nakashima H, Otaka A, Fujii N: Synthesis and evaluation of bifunctional anti-HIV agents based on specific CXCR4 antagonists-AZT conjugation. Bioorg Med Chem. 2001.08; 9 (8): 2179-2187. ( PubMed )

  5. Tamamura H, Omagari A, Hiramatsu K, Gotoh K, Kanamoto T, Xu Y, Kodama E, Matsuoka M, Hattori T, Yamamoto N, Nakashima H, Otaka A, Fujii N: Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001.07; 11 (14): 1897-1902. ( PubMed )

  6. Gotoh K, Yoshimori M, Kanbara K, Tamamura H, Kanamoto T, Mochizuki K, Fujii N, Nakashima H: Increase of R5 HIV-1 infection and CCR5 expression in T cells treated with high concentrations of CXCR4 antagonists and SDF-1. J Infect Chemother. 2001.03; 7 (1): 28-36. ( PubMed , DOI )

  7. Tamamura H, Sugioka M, Odagaki Y, Omagari A, Kan Y, Oishi S, Nakashima H, Yamamoto N, Peiper SC, Hamanaka N, Otaka A, Fujii N: Conformational study of a highly specific CXCR4 inhibitor, T140, disclosing the close proximity of its intrinsic pharmacophores associated with strong anti-HIV activity. Bioorg Med Chem Lett. 2001.02; 11 (3): 359-362. ( PubMed )

  8. Akira Otaka, Hideaki Watanabe, Akira Yukimasa, Shinya Oishi, Hirokazu Tamamura & Nobutaka Fujii: New Access to α-Substituted (Z)-Fluoroalkene Dipeptide Isosteres Utilizing Organocopper Reagents under 'Reduction-oxidative Alkylation (R-OA)' Conditions. Tetrahedron Lett.. 2001; 42 (2): 5443-5446.

  9. 玉村　啓和: HIV侵入の第二受容体に対する特異的拮抗剤の発見と応用に関する研究 薬学雑誌. 2001; 121 (11): 781-792.

  10. Kenji Kanbara, Setsuko Sato, Jun-ichi Tanuma, Hirokazu Tamamura, Kazuyo Gotoh, Manabu Yoshimori, Taisei Kanamoto, Motoo Kitano, Nobutaka Fujii & Hideki Nakashima: Biological and Genetic Characterization of a Human Immunodeficiency Virus Strain Resistant to CXCR4 Antagonist T134. AIDS Res. Hum. Retroviruses. 2001; 17 (7): 615-622.

  11. Shinya Oishi, Hirokazu Tamamura, Masaki Yamashita, Yoshihiko Odagaki, Nobuyuki Hamanaka, Akira Otaka & Nobutaka Fujii: Stereoselective Synthesis of a Set of Two Functionalized (E)-Alkene Dipeptide Isosteres of L-Amino Acid-L-Glu and L-Amino acid-D-Glu. J. Chem. Soc., Perkin Trans.. 2001; 1 (19): 2445-2451.

  1. Tamamura H, Omagari A, Oishi S, Kanamoto T, Yamamoto N, Peiper SC, Nakashima H, Otaka A, Fujii N: Pharmacophore identification of a specific CXCR4 inhibitor, T140, leads to development of effective anti-HIV agents with very high selectivity indexes. Bioorg Med Chem Lett. 2000.12; 10 (23): 2633-2637. ( PubMed )

  2. Udaka K, Wiesmuller KH, Kienle S, Jung G, Tamamura H, Yamagishi H, Okumura K, Walden P, Suto T, Kawasaki T: An automated prediction of MHC class I-binding peptides based on positional scanning with peptide libraries. Immunogenetics. 2000.08; 51 (10): 816-828. ( PubMed )

  3. Miyoshi K, Otaka A, Kaneko M, Tamamura H, Fujii N: A new practical strategy for the synthesis of long-chain phosphopeptide. Chem Pharm Bull (Tokyo). 2000.08; 48 (8): 1230-1233. ( PubMed )

  4. Otaka A, Mitsuyama E, Kinoshita T, Tamamura H, Fujii N: Stereoselective synthesis of CF(2)-substituted phosphothreonine mimetics and their incorporation into peptides using newly developed deprotection procedures. J Org Chem. 2000.08; 65 (16): 4888-4899. ( PubMed )

  5. Tamamura H, Bienfait B, Nacro K, Lewin NE, Blumberg PM, Marquez VE: Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C. J Med Chem. 2000.08; 43 (17): 3209-3217. ( PubMed )

  6. Hosoya T, Hamura T, Kuriyama Y, Miyamoto M, Matsumoto T, Suzuki K.: Silicon-Directed Regioselective [2+2] Cycloaddition of α-Alkoxybenzyne and Ketene Silyl Acetals. Synlett. 2000; (4): 520-522. ( DOI )

  7. Futagami S, Ohashi Y, Imura K, Hosoya T, Omori K, Matsumoto T, Suzuki K.: Total synthesis of ravidomycin: revision of absolute and relative stereochemistry. Tetrahedron Lett. 2000; 41 (7): 1063-1067. ( DOI )

  8. Akira Otaka, Etsuko Mitsuyama, Hideaki Watanabe, Hirokazu Tamamura & Nobutaka Fujii: Development of New Methodology for the Synthesis of Functionalized α-Fluorophosphonates and Its Practical Application to the Preparation of Phosphopeptide Mimetics. Chem. Commun.. 2000; 1081-1082.

  9. Kakugawa K, Udaka K, Nakashima K, Inaba K, Oka Y, Sugiyama H, Tamamura H, Yamagishi H: Efficient induction of peptide-specific cytotoxic T lymphocytes by LPS-activated spleen cells. Microbiol Immunol. 2000; 44 (2): 123-133. ( PubMed )

  1. Furuta K, Hosoya T, Tomokiyo K, Okuda S, Kuniyasu A, Nakayama H, Ishikawa T, Suzuki M: [35S]S-[5-(4-benzoylphenyl)pentyl]glutathione: a versatile radioligand targeting GS-X pumps with the ability of photoaffinity labeling. Bioorg Med Chem Lett. 1999.09; 9 (18): 2661-2666. ( PubMed )

  2. Murakami T, Zhang TY, Koyanagi Y, Tanaka Y, Kim J, Suzuki Y, Minoguchi S, Tamamura H, Waki M, Matsumoto A, Fujii N, Shida H, Hoxie JA, Peiper SC, Yamamoto N: Inhibitory mechanism of the CXCR4 antagonist T22 against human immunodeficiency virus type 1 infection. J Virol. 1999.09; 73 (9): 7489-7496. ( PubMed )

  3. Xu Y, Tamamura H, Arakaki R, Nakashima H, Zhang X, Fujii N, Uchiyama T, Hattori T: Marked increase in anti-HIV activity, as well as inhibitory activity against HIV entry mediated by CXCR4, linked to enhancement of the binding ability of tachyplesin analogs to CXCR4. AIDS Res Hum Retroviruses. 1999.03; 15 (5): 419-427. ( PubMed , DOI )

  4. Arakaki R, Tamamura H, Premanathan M, Kanbara K, Ramanan S, Mochizuki K, Baba M, Fujii N, Nakashima H: T134, a small-molecule CXCR4 inhibitor, has no cross-drug resistance with AMD3100, a CXCR4 antagonist with a different structure. J Virol. 1999.02; 73 (2): 1719-1723. ( PubMed )

  5. Hirokazu Tamamura, Masaki Yamashita, Yutaka Nakajima, Kyoko Sakano, Akira Otaka, Hiroaki Ohno, Toshiro Ibuka & Nobutaka Fujii: Regiospecific Ring-Opening Reactions of β-Aziridinyl α,β-Enoates with Acids: Application to the Stereoselective Synthesis of a Couple of Diastereoisomeric (E)-Alkene Dipeptide Isosteres from a Single β-Aziridinyl α,β-Enoate and to the Convenient Preparation of Amino Alcohols Bearing α,β-Unsaturated Ester Groups. J. Chem. Soc., Perkin Trans.. 1999; 1 2983-2996.

  1. Tamamura H, Xu Y, Hattori T, Zhang X, Arakaki R, Kanbara K, Omagari A, Otaka A, Ibuka T, Yamamoto N, Nakashima H, Fujii N: A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140. Biochem Biophys Res Commun. 1998.12; 253 (3): 877-882. ( PubMed , DOI )

  2. Hattori T, Komoda H, Pahwa S, Tateyama M, Zhang X, Xu Y, Oguma S, Tamamura H, Fujii N, Fukutake K, Uchiyama T: Decline of anti-DP107 antibody associated with clinical progression. AIDS. 1998.08; 12 (12): 1557-1559. ( PubMed )

  3. Tamamura H, Imai M, Ishihara T, Masuda M, Funakoshi H, Oyake H, Murakami T, Arakaki R, Nakashima H, Otaka A, Ibuka T, Waki M, Matsumoto A, Yamamoto N, Fujii N: Pharmacophore identification of a chemokine receptor (CXCR4) antagonist, T22 ([Tyr(5,12),Lys7]-polyphemusin II), which specifically blocks T cell-line-tropic HIV-1 infection. Bioorg Med Chem. 1998.07; 6 (7): 1033-1041. ( PubMed )

  4. Oguchi M, Higashi K, Taniguchi M, Nishikawa T, Tamamura H, Okimura T, Yamamoto I: Single photon emission CT images in a case of intraventricular neurocytoma. Ann Nucl Med. 1998.06; 12 (3): 161-164. ( PubMed )

  5. Tamamura H, Waki M, Imai M, Otaka A, Ibuka T, Waki K, Miyamoto K, Matsumoto A, Murakami T, Nakashima H, Yamamoto N, Fujii N: Downsizing of an HIV-cell fusion inhibitor, T22 ([Tyr5,12, Lys7]-polyphemusin II), with the maintenance of anti-HIV activity and solution structure. Bioorg Med Chem. 1998.04; 6 (4): 473-479. ( PubMed )

  6. Tamamura H, Arakaki R, Funakoshi H, Imai M, Otaka A, Ibuka T, Nakashima H, Murakami T, Waki M, Matsumoto A, Yamamoto N, Fujii N: Effective lowly cytotoxic analogs of an HIV-cell fusion inhibitor, T22 ([Tyr5,12, Lys7]-polyphemusin II). Bioorg Med Chem. 1998.02; 6 (2): 231-238. ( PubMed )

  7. Hirokazu Tamamura, Tsunehito Ishihara, Hiromi Oyake, Makoto Imai, Akira Otaka, Toshiro Ibuka, Rieko Arakaki, Hideki Nakashima, Tsutomu Murakami, Michinori Waki, Akiyoshi Matsumoto, Naoki Yamamoto & Nobutaka Fujii: Convenient One-pot Synthesis of Cystine-Containing Peptides Using the Trimethylsilyl Chloride-Dimethylsulfoxide/Trifluoroacetic Acid System and its Application to the Synthesis of Bifunctional Anti-HIV Compounds. J. Chem. Soc., Perkin Trans.. 1998; 1 (3): 495-500.

  8. Hiroaki Ohno, Kiyonori Ishii, Asami Honda, Hirokazu Tamamura, Nobutaka Fujii, Yoshiji Takemoto & Toshiro Ibuka: A 2,3-cis-Selective Synthesis of Aziridines Bearing a Vinyl Group from Allyl Methyl Carbonates and Allyl Mesylates. J. Chem. Soc., Perkin Trans.. 1998; 1 (22): 3703-3716.

  9. Uenishi H, Iwanami N, Yamagishi H, Nakatani T, Kawasaki T, Tamamura H, Fujii N, Kuribayashi K: Induction of cross-reactivity in an endogenous viral peptide non-reactive to FBL-3 tumor-specific helper T-cell clones. Microbiol Immunol. 1998; 42 (7): 479-484. ( PubMed )

  10. 玉村　啓和・藤井　信孝: Coreceptorを標的とした抗エイズ薬剤の開発状況 日本ME学会雑誌BioMedical Engineering. 1998; 12 (10): 44-51.

  1. Murakami T, Nakajima T, Koyanagi Y, Tachibana K, Fujii N, Tamamura H, Yoshida N, Waki M, Matsumoto A, Yoshie O, Kishimoto T, Yamamoto N, Nagasawa T: A small molecule CXCR4 inhibitor that blocks T cell line-tropic HIV-1 infection. J Exp Med. 1997.10; 186 (8): 1389-1393. ( PubMed )

  2. Ibuka T, Mimura N, Ohno H, Nakai K, Akaji M, Habashita H, Tamamura H, Miwa Y, Taga T, Fujii N, Yamamoto Y: Palladium(0)-Catalyzed Isomerization Reactions of Aziridines Bearing an alpha,beta-Unsaturated Ester Group: A Thermodynamic Preference for Chiral Alkyl (2E)-4,5-cis-4,5-Epimino-N-(alkyl- or arylsulfonyl) 2-Enoates over the Other Three Stereoisomers. J Org Chem. 1997.05; 62 (9): 2982-2991. ( PubMed )

  3. Hiroshi Aoyama, Norio Mimura, Hiroaki Ohno, Kiyonori Ishii, Ayako Toda, Hirokazu Tamamura, Akira Otaka, Nobutaka Fujii & Toshiro Ibuka: Regio- and Stereoselectivity in Reactions of 2,3-cis- and trans-3-Alkyl-2-vinylaziridines with Organocopper Reagents: Importance of 2,3-cis-Stereochemistry in Controlling Selectivity. Tetrahedron Lett.. 1997; 38 (42): 7383-7386.

  4. Hiroaki Ohno, Norio Mimura, Akira Otaka, Hirokazu Tamamura, Nobutaka Fujii, Toshiro Ibuka, Isao Shimizu, Akiharu Satake & Yoshinori Yamamoto: Palladium-Catalyzed Reductive Ring Opening with Formic Acid of Aziridines Bearing an α, β-Unsaturated Ester Group. Tetrahedron. 1997; 53 (38): 12933-12946.

  5. Toshiro Ibuka, Norio Mimura, Hiroshi Aoyama, Masako Akaji, Hiroaki Ohno, Yoshihisa Miwa, Tooru Taga, Kazuo Nakai, Hirokazu Tamamura, Nobutaka Fujii & Yoshinori Yamamoto: A Thermodynamic Preference of Chiral N-Methanesulfonyl and N-Arenesulfonyl 2,3-cis-3-Alkyl-2-vinylaziridines over Their 2,3-trans-Isomers: Useful Palladium(0)-Catalyzed Equilibration Reactions for the Synthesis of (E)-Alkene Dipeptide Isosters. J. Org. Chem.. 1997; 62 (4): 999-1015.

  6. Hiromu Habashita, Takeshi Kawasaki, Masako Akaji, Hirokazu Tamamura, Tetsutaro Kimachi, Nobutaka Fujii & Toshiro Ibuka: One-Pot Transformation of p-Toluenesulfonates of 2,3-Epoxy Alcohols into Allylic Alcohols. Tetrahedron Lett.. 1997; 38 (48): 8307-8310.

  1. Tamamura H, Otaka A, Murakami T, Ibuka T, Sakano K, Waki M, Matsumoto A, Yamamoto N, Fujii N: An anti-HIV peptide, T22, forms a highly active complex with Zn(II). Biochem Biophys Res Commun. 1996.12; 229 (2): 648-652. ( PubMed , DOI )

  2. Tamamura H, Ishihara T, Otaka A, Murakami T, Ibuka T, Waki M, Matsumoto A, Yamamoto N, Fujii N: Analysis of the interaction of an anti-HIV peptide, T22 ([Tyr5, 12, Lys7]-polyphemusin II), with gp120 and CD4 by surface plasmon resonance. Biochim Biophys Acta. 1996.11; 1298 (1): 37-44. ( PubMed )

  3. Tamamura H, Otaka A, Murakami T, Ishihara T, Ibuka T, Waki M, Matsumoto A, Yamamoto N, Fujii N: Interaction of an anti-HIV peptide, T22, with gp120 and CD4. Biochem Biophys Res Commun. 1996.02; 219 (2): 555-559. ( PubMed , DOI )

  4. Toshiro Ibuka, Kazuo Nakai, Masako Akaji, Hirokazu Tamamura, Nobutaka Fujii & Yoshinori Yamamoto: An Aza-Payne Rearrangement-Epoxide Ring Opening Reaction of 2-Aziridinemethanols in a One-pot Manner: A Regio- and Stereoselective Synthetic Route to Diastereomerically Pure N-Protected 1,2-Amino Alcohols. Tetrahedron. 1996; 52 11739-11752.

  5. Hosoya T, Takashiro E, Yamamoto Y, Matsumoto T, Suzuki K.: Total Syntheses of BE-12406 A and Its C(8)-Vinyl Analog. Heterocycles. 1996; 42 (1): 397-414. ( DOI )

  6. Hosoya T, Ohashi Y, Matsumoto T, Suzuki K.: On the Stereochemistry of Aryl C-Glycosides: Unusual Behavior of Bis-TBDPS Protected Aryl C-Olivosides. Tetrahedron Lett. 1996; 37 (5): 663-666. ( DOI )

  7. Hirokazu Tamamura, Tsunehito Ishihara, Akira Otaka, Takaki Koide, Kengo Miyoshi, Toshiro Ibuka & Nobutaka Fujii: A Convenient One-pot Synthesis of Cystine-Containing Peptides from Protected Peptidyl Resins Using the Trimethylsilyl Chloride-Dimethylsulfoxide-Trifluoroacetic Acid System. J. Chem. Soc., Perkin Trans. (Perkin Commun.). 1996; 1 1911-1912.

  8. Toshiro Ibuka, Masako Akaji, Norio Mimura, Hiromu Habashita, Kazuo Nakai, Hirokazu Tamamura, Nobutaka Fujii & Yoshinori Yamamoto: A Thermodynamic Preference of Chiral cis-γ,δ-Epimino-(E)-α,β-Unsaturated Esters over Other Stereoisomers: Synthetically Useful Pd(0)-Catalyzed Equilibrated Reactions of Aziridines Bearing an α,β-Unsaturated Ester Groups. Tetrahedron Lett.,. 1996; 37 2849-2852.

  9. Norio Mimura, Toshiro Ibuka, Masako Akaji, Yoshihisa Miwa, Tooru Taga, Kazuo Nakai, Hirokazu Tamamura, Nobutaka Fujii & Yoshinori Yamamoto: An Unusual Thermodynamic Preference of Chiral N-Arylsulfonyl cis-3-Alkyl-2-vinylaziridines over Their trans-Isomers: Palladium(0)-Catalyzed Equilibration Reaction. J. Chem. Soc., Chem. Commun.. 1996; 351-352.

  10. Nobutaka Fujii, Hiromu Habashita, Masako Akaji, Kazuo Nakai, Toshiro Ibuka, Masahiro Fujiwara, Hirokazu Tamamura & Yoshinori Yamamoto: A Simple One-pot Transformation of p-Toluenesulfonates of 2,3-Epoxy Alcohols into Allylic Alcohols. J. Chem. Soc., Perkin Trans. (Perkin Commun.). 1996; 1 1996, 865-866.

  11. Michinori Waki, Koji Waki, Kenji Miyamoto, Akiyoshi Matsumoto, Hirokazu Tamamura, Nobutaka Fujii, Tsutomu Murakami, Hideki Nakashima & Naoki Yamamoto: Molecular Size of an Anti-HIV Peptide, T22, Can Be Reduced without Loss of the Activity. Chem. Lett.. 1996; 571-572.

  1. Kondo T, Uenishi H, Shimizu T, Hirama T, Iwashiro M, Kuribayashi K, Tamamura H, Fujii N, Fujisawa R, Miyazawa M, et al.: A single retroviral gag precursor signal peptide recognized by FBL-3 tumor-specific cytotoxic T lymphocytes. J Virol. 1995.11; 69 (11): 6735-6741. ( PubMed )

  2. Weeks BS, Nomizu M, Otaka A, Weston CA, Okusu A, Tamamura H, Yamamoto N, Fujii N: The synthetic [Tyr5,12,Lys7]-polyphemusin II peptide (T22) binds to the CD4 cell surface molecule. Biochem Biophys Res Commun. 1995.10; 215 (2): 626-631. ( PubMed , DOI )

  3. Tamamura H, Murakami T, Horiuchi S, Sugihara K, Otaka A, Takada W, Ibuka T, Waki M, Yamamoto N, Fujii N: Synthesis of protegrin-related peptides and their antibacterial and anti-human immunodeficiency virus activity. Chem Pharm Bull (Tokyo). 1995.05; 43 (5): 853-858. ( PubMed )

  4. Tamamura H, Otaka A, Nakamura J, Okubo K, Koide T, Ikeda K, Ibuka T, Fujii N: Disulfide bond-forming reaction using a dimethyl sulfoxide/aqueous HCl system and its application to regioselective two disulfide bond formation. Int J Pept Protein Res. 1995.04; 45 (4): 312-319. ( PubMed )

  5. Tamamura H, Otaka A, Takada W, Terakawa Y, Yoshizawa H, Masuda M, Ibuka T, Murakami T, Nakashima H, Waki M, et al.: Solution-phase synthesis of an anti-human immunodeficiency virus peptide, T22 ([Tyr5,12,Lys7]-polyphemusin II), and the modification of Trp by the p-methoxybenzyl group of Cys during trimethylsilyl trifluoromethanesulfonate deprotection. Chem Pharm Bull (Tokyo). 1995.01; 43 (1): 12-18. ( PubMed )

  6. Akira Otaka, Kengo Miyoshi, Terrence R. Burke, Jr., Peter P. Roller, Hideki Kubota, Hirokazu Tamamura & Nobutaka Fujii: Synthesis and Application of N-Boc-L-2-amino-4-(diethylphosphono)-4, 4-difluorobutanoic acid for Solid-Phase Synthesis of Nonhydrolyzable Phosphoserine Peptide Analogs. Tetrahedron Lett.. 1995; 36 927-930.

  7. Akira Otaka, Kengo Miyoshi, Peter P. Roller, Terrence R. Burke, Jr., Hirokazu Tamamura & Nobutaka Fujii: Practical Synthesis of Phosphopeptides using Dimethyl-protected Phosphoamino Acid Derivatives. J. Chem. Soc., Chem. Commun.. 1995; 387-389.

  8. Hosoya T, Hasegawa T, Kuriyama Y, Suzuki K: Stereospecificity in [2 + 2] Cycloaddition of Benzyne and Ketene Silyl Acetal. Tetrahedron Lett. 1995; 36 (19): 3377-3380. ( DOI )

  9. Suzuki K, Matsumoto T, Hosoya T.: Total Synthesis of the Gilvocarcins. J Synth Org Chem, Jpn. 1995; 53 (11): 1045-1054.

  10. Hosoya T, Hasegawa T, Kuriyama Y, Matsumoto T, Suzuki K.: [2 + 2] Cycloaddition of Benzyne and Ketene Silyl Acetal as an Efficient Route to Benzocyclobutenones. Synlett. 1995; (2): 177-179. ( DOI )

  11. Hosoya T, Kuriyama Y, Suzuki K.: Convenient Synthesis of Phthalides via Regioselective Baeyer-Villiger Oxidation of Benzocyclobutenones. Synlett. 1995; (6): 635-638. ( DOI )

  12. Nobutaka Fujii, Kazuo Nakai, Hirokazu Tamamura, Akira Otaka, Norio Mimura, Yoshihisa Miwa, Tooru Taga, Yoshinori Yamamoto & Toshiro Ibuka: SN2' Ring Opening of Aziridines Bearing an α,β-Unsaturated Ester Group with Organocopper Reagents. A New Stereoselective Synthesis Route to (E)-Alkene Dipeptide Isosters. J. Chem. Soc., Perkin Trans.. 1995; 1 1359-1371.

  13. Akira Otaka, Kengo Miyoshi, Midori Kaneko, Hirokazu Tamamura, Nobutaka Fujii, Motoyoshi Nomizu, Terrence R. Burke, Jr. & Peter P. Roller: Development of Efficient Two-Step Deprotection Methodology for Dimethyl-Protected Phosphoamino Acid-Containing Peptide Resins and Its Application to the Practical Synthesis of Phosphopeptides. J. Org. Chem.. 1995; 60 3967-3974.

  14. Toshiro Ibuka, Kazuo Nakai, Hiromu Habashita, Yuka Hotta, Akira Otaka, Hirokazu Tamamura, Nobutaka Fujii, Norio Mimura, Yoshihisa Miwa, Tooru Taga, Yukiyasu Chounan & Yoshinori Yamamoto: Aza-Payne Rearrangement of Activated 2-Aziridinemethanols and 2,3-Epoxy Amines under Basic Conditions. J.Org.Chem.. 1995; 60 2044-2058.

  15. Kazuo Nakai, Toshiro Ibuka, Akira Otaka, Hirokazu Tamamura, Nobutaka Fujii & Yoshinori Yamamoto: A One-pot Aza-Payne Rearrangement-Epoxide Ring Opening Reaction of 2-Aziridinemethanols: A Regio- and Stereoselective Synthetic Route to Diastereomerically Pure 1,2-Amino Alcohols. Tetrahedron Lett.. 1995; 36 6247-6250.

  1. Tamamura H, Murakami T, Masuda M, Otaka A, Takada W, Ibuka T, Nakashima H, Waki M, Matsumoto A, Yamamoto N, et al.: Structure-activity relationships of an anti-HIV peptide, T22. Biochem Biophys Res Commun. 1994.12; 205 (3): 1729-1735. ( PubMed )

  2. Otaka A, Tamamura H, Terakawa Y, Masuda M, Koide T, Murakami T, Nakashima H, Matsuzaki K, Miyajima K, Ibuka T, et al.: Molecular parameters for the anti-human immunodeficiency virus activity of T22 ([Tyr5,12, Lys7]-polyphemusin II). Biol Pharm Bull. 1994.12; 17 (12): 1669-1672. ( PubMed )

  3. Shimizu T, Uenishi H, Teramura Y, Iwashiro M, Kuribayashi K, Tamamura H, Fujii N, Yamagishi H: Fine structure of a virus-encoded helper T-cell epitope expressed on FBL-3 tumor cells. J Virol. 1994.12; 68 (12): 7704-7708. ( PubMed )

  4. Weeks BS, Nomizu M, Otaka A, Weston CA, Okusu A, Tamamura H, Matsumoto A, Yamamoto N, Fujii N: Lymphocytes and promonocytes attach to the synthetic [Tyr5,12, Lys7]- polyphemusin II peptide. Biochem Biophys Res Commun. 1994.07; 202 (1): 470-475. ( PubMed )

  5. Hosoya T, Takashiro E, Matsumoto T, Suzuki K.: Total Synthesis of the Gilvocarcins. J Am Chem Soc. 1994; 116 (3): 1004-1015. ( DOI )

  6. Hosoya T, Takashiro E, Matsumoto T, Suzuki K.: First Total Synthesis of BE-12406 A. Tetrahedron Lett. 1994; 35 (26): 4591-4594. ( DOI )

  7. Nobutaka Fujii, Kazuo Nakai, Hiromu Habashita, Yuka Hotta, Hirokazu Tamamura, Akira Otaka & Toshiro Ibuka: Synthesis of Optically Pure 2-Aziridinemethanols: Versatile Synthetic Building Blocks. Chem. Pharm. Bull.. 1994; 42 2241-2250.

  8. Toshiro Ibuka, Keisuke Suzuki, Hiromu Habashita, Akira Otaka, Hirokazu Tamamura, Norio Mimura, Yoshihisa Miwa, Tooru Taga & Nobutaka Fujii: (E)-Stereoselective Synthesis of Vinylglycines from (R)-Serine via Organocopper-BF3 and Related Reagents. J. Chem. Soc., Chem. Commun.. 1994; 2151-2152.

  1. Tamamura H, Kuroda M, Masuda M, Otaka A, Funakoshi S, Nakashima H, Yamamoto N, Waki M, Matsumoto A, Lancelin JM, et al.: A comparative study of the solution structures of tachyplesin I and a novel anti-HIV synthetic peptide, T22 ([Tyr5,12, Lys7]-polyphemusin II), determined by nuclear magnetic resonance. Biochim Biophys Acta. 1993.05; 1163 (2): 209-216. ( PubMed )

  2. Tamamura H, Ikoma R, Niwa M, Funakoshi S, Murakami T, Fujii N: Antimicrobial activity and conformation of tachyplesin I and its analogs. Chem Pharm Bull (Tokyo). 1993.05; 41 (5): 978-980. ( PubMed )

  3. Tamamura H, Nakamura J, Noguchi K, Funakoshi S, Fujii N: Acceleration of the N alpha-deprotection rate by the addition of m-cresol to diluted methanesulfonic acid and its application to the Z(OMe)-based solid-phase syntheses of human pancreastatin-29 and magainin 1. Chem Pharm Bull (Tokyo). 1993.05; 41 (5): 954-957. ( PubMed )

  4. Toshiro Ibuka, Tooru Taga, Hiromu Habashita, Kazuo Nakai, Hirokazu Tamamura, Nobutaka Fujii, Yukiyasu Chounan, Hisao Nemoto & Yoshinori Yamamoto : Syn-SN2' Pathway in the Reaction of Certain γ-(Mesyloxy)-α,β-Enoates with RCu(CN)MgX.BF3 Reagents. Importance of MgX and Bulky R Group upon the Diastereoselectivity. J. Org. Chem.. 1993; 58 1207-1214.

  5. Hirokazu Tamamura, Akira Otaka, Junko Nakamura, Kaori Okubo, Takaki Koide, Kyoko Ikeda & Nobutaka Fujii.: Disulfide Bond Formation in S-Acetamidomethyl Cysteine-Containing Peptides by the Combination of Silver Trifluoromethanesulfonate and Dimethylsulfoxide / Aqueous HCl. Tetrahedron Lett.. 1993; 34 4931-4934.

  1. Masuda M, Nakashima H, Ueda T, Naba H, Ikoma R, Otaka A, Terakawa Y, Tamamura H, Ibuka T, Murakami T, et al.: A novel anti-HIV synthetic peptide, T-22 ([Tyr5,12,Lys7]-polyphemusin II). Biochem Biophys Res Commun. 1992.12; 189 (2): 845-850. ( PubMed )

  2. Matsumoto T, Hosoya T, Suzuki K.: Total Synthesis and Absolute Stereochemical Assignment of Gilvocarcin M. J Am Chem Soc. 1992; 114 (9): 3568-3570. ( DOI )

  1. Matsumoto T, Hosoya T, Katsuki M, Suzuki K.: New Efficient Protocol for Aryne Generation. Selective Synthesis of Differentially Protected 1,4,5-Naphthalenetriols. Tetrahedron Lett. 1991; 32 (46): 6735-6736. ( DOI )

  2. Matsumoto T, Hosoya T, Suzuki K.: O->C-Glycoside Rearrangement of Resorcinol Derivatives. Versatile Intermediates in the Synthesis of Aryl C-Glycosides. Synlett. 1991; (10): 709-711. ( DOI )

  1. Miyasaka K, Funakoshi A, Kitani K, Tamamura H, Funakoshi S, Fujii N: Inhibitory effect of pancreastatin on pancreatic exocrine secretions. Pancreastatin inhibits central vagal nerve stimulation. Gastroenterology. 1990.12; 99 (6): 1751-1756. ( PubMed )

  2. Tamamura H, Ohta M, Yoshizawa K, Ono Y, Funakoshi A, Miyasaka K, Tateishi K, Jimi A, Yajima H, Fujii N, et al.: Isolation and characterization of a tumor-derived human protein related to chromogranin A and its in vitro conversion to human pancreastatin-48. Eur J Biochem. 1990.07; 191 (1): 33-39. ( PubMed )

  3. Miyasaka K, Funakoshi A, Yasunami Y, Nakamura R, Kitani K, Tamamura H, Funakoshi S, Fujii N: Rat pancreastatin inhibits both pancreatic exocrine and endocrine secretions in rats. Regul Pept. 1990.04; 28 (2): 189-198. ( PubMed )

  4. Miyasaka K, Funakoshi A, Kitani K, Tamamura H, Fujii N, Funakoshi S: The importance of the C-terminal amide structure of rat pancreastatin to inhibit pancreatic exocrine secretion. FEBS Lett. 1990.04; 263 (2): 279-280. ( PubMed )

  5. Matsumoto T, Hosoya T, Suzuki K.: Improvement in O->C-Glycoside Rearrangement Approach to C-Aryl Glycosides: Use of 1-O-Acetyl Sugar as Stable but Efficient Glycosyl Donor. Tetrahedron Lett. 1990; 31 (32): 4629-4632. ( DOI )

  6. Akihiro Funakoshi, Kyoko Miyasaka, Kenichi Kitani, Susumu Funakoshi, Hirokazu Tamamura, Nobutaka Fujii, Itsuro Nakano & Kazuhiko Tatemoto: Comparative Effects of Mammalian Pancreastatin on the Pancreatic Exocrine Secretion. Japanese J. Pysiol.. 1990; 39 901-905.

  1. Tateishi K, Funakoshi A, Wakasugi H, Iguchi H, Shinozaki H, Abe M, Funakoshi S, Tamamura H, Yajima H, Matsuoka Y: Plasma pancreastatin-like immunoreactivity in various diseases. J Clin Endocrinol Metab. 1989.12; 69 (6): 1305-1308. ( PubMed )

  2. Tateishi K, Funakoshi A, Jimi A, Funakoshi S, Tamamura H, Yajima H, Matsuoka Y: High plasma pancreastatinlike immunoreactivity in a patient with malignant insulinoma. Gastroenterology. 1989.11; 97 (5): 1313-1318. ( PubMed )

  3. Funakoshi S, Tamamura H, Ohta M, Yoshizawa K, Funakoshi A, Miyasaka K, Tateishi K, Tatemoto K, Nakano I, Yajima H, et al.: Isolation and characterization of a tumor-derived human pancreastatin-related protein. Biochem Biophys Res Commun. 1989.10; 164 (1): 141-148. ( PubMed )

  4. Funakoshi A, Jimi A, Yasunami Y, Tateishi K, Funakoshi S, Tamamura H, Yajima H: Bioactivity of human pancreastatin and its localization in pancreas. Biochem Biophys Res Commun. 1989.03; 159 (3): 913-918. ( PubMed )

  5. Funakoshi A, Miyasaka K, Kitani K, Tamamura H, Funakoshi S, Yajima H: Bioactivity of synthetic C-terminal fragment of rat pancreastatin on endocrine pancreas. Biochem Biophys Res Commun. 1989.02; 158 (3): 844-849. ( PubMed )

  6. Nobutaka Fujii, Akira Otaka, Toshihiro Watanabe, Akira Okamachi, Hirokazu Tamamura, Haruaki Yajima, Yoshimasa Inagaki, Motoyoshi Nomizu & Katsuhiko Asano: Silver Trifluoromethanesulphonate as an S-Deprotecting Reagent for the Synthesis of Cystine Peptides. J. Chem. Soc., Chem. Commun.. 1989; 283-284.

  1. Funakoshi A, Miyasaka K, Nakamura R, Kitani K, Funakoshi S, Tamamura H, Fujii N, Yajima H: Bioactivity of synthetic human pancreastatin on exocrine pancreas. Biochem Biophys Res Commun. 1988.11; 156 (3): 1237-1242. ( PubMed )

  2. Susumu Funakoshi, Hirokazu Tamamura, Nobutaka Fujii, Kumi Yoshizawa, Haruaki Yajima, Kyoko Miyasaka, Akihiro Funakoshi, Mitsuhiro Ohta, Yoshimasa Inagaki & Louis A. Carpino: Combination of a New Amide-precursor Reagent and Trimethylsilyl Bromide Deprotection for the Fmoc-based Solid Phase Synthesis of Human Pancreastatin and One of its Fragment. J. Chem. Soc., Chem. Commun.. 1988; 1588-1590.

  1. Yamashita Yasunobu, Takada Yuri, Itoh Yukihiro, Suzuki Takayoshi: Discovery of HDAC8-selective inhibitors and their application to PROTACs MEDCHEM NEWS. 2023.11; 33 (4): 181-186. ( DOI )

  1. Takuya Kobayakawa, Hirokazu Tamamura: Development for peptidomimetic chemistry based on chloroalkene structures Journal of Synthetic Organic Chemistry, Japan. 2019.09; 77 (9): 904-911.

  2. Takuya Kobayakawa: Development for peptidomimetic chemistry utilizing the oxetanyl structure Journal of Synthetic Organic Chemistry, Japan; Review de Debut. 2019.07; 77 (7): 720-721.

  3. Toru Komatsu, Yukihiro Itoh: Challenges of young chemists to be global Yakugaku Zasshi. 2019; 139 (2): 185-186. ( PubMed , DOI )

  1. Tsukamoto S., Sakae Y., Itoh Y., Suzuki T., Okamoto Y.: 22aPS-113 Study on the selectivity of the epigenetic enzyme inhibitor by generalized-ensemble molecular dynamics simulations Meeting Abstracts of the Physical Society of Japan. 2016; 71 3323. ( DOI )

  1. Shinya Fujii, Aya Tanatani, Tomoya Hirano, Hiroyuki Kagechika: Development of nonsecosteroidal vitamin D derivatives bearing carborane as hydrophobic pharmacophore 2014; 88 389-395.

  2. Minoru Imai, Hiroyuki Kagechika: Develpmnt of anticancer drugs targeting retinoid nuclear receptors 2014; 249 1189-1193.

  3. Mari Yuasa, Hiroyuki Kagechika: Tecknology in Chemical Biology Research 2014; 53 407-410.

  4. Hiroyuki Kagechika: medicinal chemistry of nuclear receptors 2014; 32 299-305.

  1. HDAC6-selective inhibitors 2008.01; 224 (1): 71-74.

  1. Anirban Mukherjee, Yasunobu Yamashita, Ryo Maeda, Toshiki Akiyama, Katsunori Endo, Yuri Takada, Hiroki Tsumoto, Yukiko Moriyama, Akihiro Ito, Fumiyuki Shirai, Makoto Tachibana, Yukihiro Itoh, Takayoshi Suzuki: A Novel PROTAC G9a/GLP Degrader that Inhibits, Similar to G9a siRNA, the Migration of MCF-7 Breast-Cancer Cells without Affecting Proliferation Journal of Medicinal Chemistry. 2025.09; 68 (17): 18258-18271. ( PubMed , DOI )

  2. Yasunobu Yamashita, Yuuki Taki, Yoshinori Wakabayashi, Junichiro Kanazawa, Paddy R. A. Melsen, Yuri Takada, Yukihiro Itoh, Masanobu Uchiyama, Takayoshi Suzuki: A Deep-Learning-Aided Drug Screening Based on Visualization of a Hidden Layer as Chemical Space ACS Medicinal Chemistry Letters. 2025.06; ( DOI )

  1. Tetsuya Iida, Yukihiro Itoh, Yukari Takahashi, Yuka Miyake, Farzad Zamani, Yasunobu Yamashita, Yuri Takada, Toshiki Akiyama, Jun Ibaraki, Kyoka Okuda, Yuto Tokuda, Tomoka Nishimura, Koto Hidaka, Hiiro Mori, Makoto Oba, Takayoshi Suzuki: Identification of Proteolysis Targeting Chimeras (PROTACs) for Lysine Demethylase 5 and Their Neurite Outgrowth-Promoting Activity Chemical and Pharmaceutical Bulletin. 2024.07; 72 (7): 638-647. ( DOI )

  2. Hiroyuki Baba, Tadashi Hosoya, Ryosuke Ishida, Kenpei Tai, Saki Hatsuzawa, Yuma Kondo, Hiroyuki Kusuhara, Hiroyuki Kagechika, Shinsuke Yasuda: Anti-Inflammatory Effects of a Novel Nuclear Factor–κB Inhibitory Derivative Derived from Pyrazolo[3,4-d]Pyrimidine in Three Inflammation Models Journal of Pharmacology and Experimental Therapeutics. 2024.03; 388 (3): 788-797. ( DOI )

  3. 伊藤幸裕, 高田悠里, 山下泰信, 鈴木孝禎: Drug modalities for inhibition of protein-protein interactions 実験医学. 2024; 42 (2):

  1. Yukihiro Itoh, Peng Zhan, Toshifumi Tojo, Pattaporn Jaikhan, Yosuke Ota, Miki Suzuki, Ying Li, Zi Hui, Yukiko Moriyama, Yuri Takada, Yasunobu Yamashita, Makoto Oba, Shusaku Uchida, Mitsuharu Masuda, Shinji Ito, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki: Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation Journal of Medicinal Chemistry. 2023.10; 66 (22): 15171-15188. ( PubMed , DOI )

  1. Yuri Takada, Yasunobu Yamashita, Yukihiro Itoh, Takayoshi Suzuki: Medicinal Chemistry Research on Targeting Epigenetic Complexes Journal of Synthetic Organic Chemistry, Japan. 2022.07; 80 (7): 664-675. ( DOI )

  1. Yukihiro Itoh, Takashi Kurohara, Takayoshi Suzuki: N+-C-H…O Hydrogen Bonds in Protein-Ligand Complexes and their Application to Drug Design Journal of Synthetic Organic Chemistry, Japan. 2020.12; 78 (12): 1151-1162. ( DOI )

  2. Yuka Miyake, Yukihiro Itoh, Yoshinori Suzuma, Hidehiko Kodama, Takashi Kurohara, Yasunobu Yamashita, Remy Narozny, Yutaro Hanatani, Shusaku Uchida, Takayoshi Suzuki: Metalloprotein-Catalyzed Click Reaction for In Situ Generation of a Potent Inhibitor ACS Catalysis. 2020.04; 10 (10): 5383-5392. ( DOI )

  1. Keiichiro Okuhira, Takuji Shoda, Risa Omura, Nobumichi Ohoka, Takayuki Hattori, Norihito Shibata, Yosuke Demizu, Ryo Sugihara, Asato Ichino, Haruka Kawahara, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Masaaki Kurihara, Susumu Itoh, Hiroyuki Saito, Mikihiko Naito: Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules Molecular Pharmacology. 2017.03; 91 (3): 159-166. ( PubMed , DOI )

  2. Paolo Mellini, Yukihiro Itoh, Hiroki Tsumoto, Ying Li, Miki Suzuki, Natsuko Tokuda, Taeko Kakizawa, Yuri Miura, Jun Takeuchi, Maija Lahtela-Kakkonen, Takayoshi Suzuki: Potent mechanism-based sirtuin-2-selective inhibition by an: In situ -generated occupant of the substrate-binding site, "selectivity pocket" and NAD+-binding site Chemical Science. 2017; 8 (9): 6400-6408. ( PubMed , DOI )

  3. Yukihiro Itoh, Takayoshi Suzuki: “Drug" discovery with the help of organic chemistry Yakugaku Zasshi. 2017; 137 (3): 283-292. ( PubMed , DOI )

  4. Youhei Sohma, Yukihiro Itoh: Chemical biology for pharmaceutical sciences (novel ideas for “drug" discovery) Yakugaku Zasshi. 2017; 137 (3): 281-282. ( PubMed , DOI )

  1. Fumihiro Higuchi, Shusaku Uchida, Hirotaka Yamagata, Naoko Abe-Higuchi, Teruyuki Hobara, Kumiko Hara, Ayumi Kobayashi, Tatsushi Shintaku, Yukihiro Itoh, Takayoshi Suzuki, Yoshifumi Watanabe: Hippocampal microRNA-124 enhances chronic stress resilience in mice Journal of Neuroscience. 2016.07; 36 (27): 7253-7267. ( PubMed , DOI )

  2. Taeko Kakizawa, Tamio Mizukami, Yukihiro Itoh, Makoto Hasegawa, Ryuzo Sasaki, Takayoshi Suzuki: Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide Bioorganic and Medicinal Chemistry Letters. 2016.02; 26 (4): 1193-1195. ( PubMed , DOI )

  3. Yukihiro Itoh, Keisuke Aihara, Paolo Mellini, Toshifumi Tojo, Yosuke Ota, Hiroki Tsumoto, Viswas Raja Solomon, Peng Zhan, Miki Suzuki, Daisuke Ogasawara, Akira Shigenaga, Tsubasa Inokuma, Hidehiko Nakagawa, Naoki Miyata, Tamio Mizukami, Akira Otaka, Takayoshi Suzuki: Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators Journal of Medicinal Chemistry. 2016.02; 59 (4): 1531-1544. ( PubMed , DOI )

  4. Yosuke Ota, Yukihiro Itoh, Asako Kaise, Kiminori Ohta, Yasuyuki Endo, Mitsuharu Masuda, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki: Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen Angewandte Chemie - International Edition. 2016; 55 (52): 16115-16118. ( PubMed , DOI )

  5. Yukihiro Itoh, Miki Suzuki, Taiji Matsui, Yosuke Ota, Zi Hui, Kazunori Tsubaki, Takayoshi Suzuki: False HDAC inhibition by aurone compound Chemical and Pharmaceutical Bulletin. 2016; 64 (8): 1124-1128. ( PubMed , DOI )

  6. Shin Miyamura, Misaho Araki, Yosuke Ota, Yukihiro Itoh, Shusuke Yasuda, Mitsuharu Masuda, Tomoyuki Taniguchi, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki, Kenichiro Itami, Junichiro Yamaguchi: C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors Organic and Biomolecular Chemistry. 2016; 14 (36): 8576-8585. ( PubMed , DOI )

  7. Yukihiro Itoh, Takayoshi Suzuki: Molecular technology for controlling epigenetics: Regulation of histone acetylation and methylation by small molecules Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry. 2016; 74 (5): 441-452. ( DOI )

  1. Yukihiro Itoh, Hideyuki Sawada, Miki Suzuki, Toshifumi Tojo, Ryuzo Sasaki, Makoto Hasegawa, Tamio Mizukami, Takayoshi Suzuki: Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells ACS Medicinal Chemistry Letters. 2015.06; 6 (6): 665-670. ( PubMed , DOI )

  2. Taeko Kakizawa, Yosuke Ota, Yukihiro Itoh, Hiroki Tsumoto, Takayoshi Suzuki: Histone H3 peptide based LSD1-selective inhibitors Bioorganic and Medicinal Chemistry Letters. 2015.05; 25 (9): 1925-1928. ( PubMed , DOI )

  3. Mohammed Naseer Ahmed Khan, Hiroki Tsumoto, Yukihiro Itoh, Yosuke Ota, Miki Suzuki, Daisuke Ogasawara, Hidehiko Nakagawa, Tamio Mizukami, Naoki Miyata, Takayoshi Suzuki: Design, synthesis, and biological activity of N-alkylated analogue of NCL1, a selective inhibitor of lysine-specific demethylase 1 MedChemComm. 2015.03; 6 (3): 407-412. ( DOI )

  1. Peng Zhan, Yu'Ning Song, Yukihiro Itoh, Takayoshi Suzuki, Xinyong Liu: Recent advances in the structure-based rational design of TNKSIs Molecular BioSystems. 2014.11; 10 (11): 2783-2799. ( PubMed , DOI )

  2. Hiromi Sekizawa, Kazuma Amaike, Yukihiro Itoh, Takayoshi Suzuki, Kenichiro Itami, Junichiro Yamaguchi: Late-stage C-H coupling enables rapid identification of HDAC inhibitors: Synthesis and evaluation of NCH-31 analogues ACS Medicinal Chemistry Letters. 2014.05; 5 (5): 582-586. ( PubMed , DOI )

  3. Prima R. Tatum, Hideyuki Sawada, Yosuke Ota, Yukihiro Itoh, Peng Zhan, Naoya Ieda, Hidehiko Nakagawa, Naoki Miyata, Takayoshi Suzuki: Identification of novel SIRT2-selective inhibitors using a click chemistry approach Bioorganic and Medicinal Chemistry Letters. 2014.04; 24 (8): 1871-1874. ( PubMed , DOI )

  4. Takayoshi Suzuki, Nobusuke Muto, Masashige Bando, Yukihiro Itoh, Ayako Masaki, Masaki Ri, Yosuke Ota, Hidehiko Nakagawa, Shinsuke Iida, Katsuhiko Shirahige, Naoki Miyata: Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylasea 8-selective inhibitors ChemMedChem. 2014.03; 9 (3): 657-664. ( PubMed , DOI )

  5. Yukihiro Itoh, Naoki Miyata, Takayoshi Suzuki: Target-guided synthesis: Medicinal chemistry strategy to allow target enzymes themselves to synthesize their own inhibitors Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry. 2014; 72 (6): 702-716. ( DOI )

  6. Yukihiro Itoh, Daisuke Ogasawara, Yosuke Ota, Tamio Mizukami, Takayoshi Suzuki: Synthesis, LSD1 inhibitory activity, and LSD1 Binding model of optically pure lysine-PCPA conjugates Computational and Structural Biotechnology Journal. 2014; 9 (14): e201402002. ( PubMed , DOI )

  1. Yuji Matsuya, Yuta Kobayashi, Sayumi Uchida, Yukihiro Itoh, Hideyuki Sawada, Takayoshi Suzuki, Naoki Miyata, Kenji Sugimoto, Naoki Toyooka: Search for a novel SIRT1 activator: Structural modification of SRT1720 and biological evaluation Bioorganic and Medicinal Chemistry Letters. 2013.09; 23 (17): 4907-4910. ( PubMed , DOI )

  2. Takayoshi Suzuki, Hiroki Ozasa, Yukihiro Itoh, Peng Zhan, Hideyuki Sawada, Koshiki Mino, Louise Walport, Rei Ohkubo, Akane Kawamura, Masato Yonezawa, Yuichi Tsukada, Anthony Tumber, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Christopher J. Schofield, Naoki Miyata: Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity Journal of Medicinal Chemistry. 2013.09; 56 (18): 7222-7231. ( PubMed , DOI )

  3. Daisuke Ogasawara, Yukihiro Itoh, Hiroki Tsumoto, Taeko Kakizawa, Koshiki Mino, Kiyoshi Fukuhara, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata, Takayoshi Suzuki: Lysine-specific demethylase 1-selective inactivators: Protein-targeted drug delivery mechanism Angewandte Chemie - International Edition. 2013.08; 52 (33): 8620-8624. ( PubMed , DOI )

  4. Takayoshi Suzuki, Yuki Kasuya, Yukihiro Itoh, Yosuke Ota, Peng Zhan, Kaori Asamitsu, Hidehiko Nakagawa, Takashi Okamoto, Naoki Miyata: Identification of Highly Selective and Potent Histone Deacetylase 3 Inhibitors Using Click Chemistry-Based Combinatorial Fragment Assembly PLoS ONE. 2013.07; 8 (7): e68669. ( PubMed , DOI )

  5. Yukihiro Itoh, Takayoshi Suzuki, Naoki Miyata: Small-molecular modulators of cancer-associated epigenetic mechanisms Molecular BioSystems. 2013.05; 9 (5): 873-896. ( PubMed , DOI )

  1. Takayoshi Suzuki, Yosuke Ota, Masaki Ri, Masashige Bando, Aogu Gotoh, Yukihiro Itoh, Hiroki Tsumoto, Prima R. Tatum, Tamio Mizukami, Hidehiko Nakagawa, Shinsuke Iida, Ryuzo Ueda, Katsuhiko Shirahige, Naoki Miyata: Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries Journal of Medicinal Chemistry. 2012.11; 55 (22): 9562-9575. ( PubMed , DOI )

  2. Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Keiichiro Okuhira, Mikihiko Naito, Yuichi Hashimoto: Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist Bioorganic and Medicinal Chemistry Letters. 2012.07; 22 (13): 4453-4457. ( PubMed , DOI )

  3. Takayoshi Suzuki, Mohammed Naseer Ahmed Khan, Hideyuki Sawada, Erika Imai, Yukihiro Itoh, Katsura Yamatsuta, Natsuko Tokuda, Jun Takeuchi, Takuya Seko, Hidehiko Nakagawa, Naoki Miyata: Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors Journal of Medicinal Chemistry. 2012.06; 55 (12): 5760-5773. ( PubMed , DOI )

  1. Yukihiro Itoh, Risa Kitaguchi, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto: Design, synthesis and biological evaluation of nuclear receptor-degradation inducers Bioorganic and Medicinal Chemistry. 2011.11; 19 (22): 6768-6778. ( PubMed , DOI )

  2. Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto: Development of target protein-selective degradation inducer for protein knockdown Bioorganic and Medicinal Chemistry. 2011.05; 19 (10): 3229-3241. ( PubMed , DOI )

  3. Keiichiro Okuhira, Nobumichi Ohoka, Kimie Sai, Tomoko Nishimaki-Mogami, Yukihiro Itoh, Minoru Ishikawa, Yuichi Hashimoto, Mikihiko Naito: Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein FEBS Letters. 2011.04; 585 (8): 1147-1152. ( PubMed , DOI )

  1. Shohei Hamada, Takayoshi Suzuki, Koshiki Mino, Koichi Koseki, Felix Oehme, Ingo Flamme, Hiroki Ozasa, Yukihiro Itoh, Daisuke Ogasawara, Haruka Komaarashi, Aiko Kato, Hiroki Tsumoto, Hidehiko Nakagawa, Makoto Hasegawa, Ryuzo Sasaki, Tamio Mizukami, Naoki Miyata: Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors Journal of Medicinal Chemistry. 2010.08; 53 (15): 5629-5638. ( PubMed , DOI )

  2. Yukihiro Itoh, Minoru Ishikawa, Mikihiko Naito, Yuichi Hashimoto: Protein knockdown using methyl bestatin-ligand hybrid molecules: Design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins Journal of the American Chemical Society. 2010.04; 132 (16): 5820-5826. ( PubMed , DOI )

  1. Shohei Hamada, Tae Dong Kim, Takayoshi Suzuki, Yukihiro Itoh, Hiroki Tsumoto, Hidehiko Nakagawa, Ralf Janknecht, Naoki Miyata: Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors Bioorganic and Medicinal Chemistry Letters. 2009.05; 19 (10): 2852-2855. ( PubMed , DOI )

  1. Takayoshi Suzuki, Sou Ichi Igari, Akira Hirasawa, Mie Hata, Masaji Ishiguro, Hiroki Fujieda, Yukihiro Itoh, Tatsuya Hirano, Hidehiko Nakagawa, Michitaka Ogura, Makoto Makishima, Gozoh Tsujimoto, Naoki Miyata: Identification of G protein-coupled receptor 120-selective agonists derived from PPARγ agonists Journal of Medicinal Chemistry. 2008.12; 51 (23): 7640-7644. ( PubMed , DOI )

  2. Yukihiro Itoh, Takayoshi Suzuki, Naoki Miyata: Isoform-selective histone deacetylase inhibitors Current Pharmaceutical Design. 2008.02; 14 (6): 529-544. ( PubMed , DOI )

  1. Yukihiro Itoh, Takayoshi Suzuki, Akiyasu Kouketsu, Nobuaki Suzuki, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata: Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors Journal of Medicinal Chemistry. 2007.11; 50 (22): 5425-5438. ( PubMed , DOI )

  2. Takayoshi Suzuki, Shinya Hisakawa, Yukihiro Itoh, Nobuaki Suzuki, Katsumasa Takahashi, Masatoshi Kawahata, Kentaro Yamaguchi, Hidehiko Nakagawa, Naoki Miyata: Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors Bioorganic and Medicinal Chemistry Letters. 2007.08; 17 (15): 4208-4212. ( PubMed , DOI )

  3. Takayoshi Suzuki, Shinya Hisakawa, Yukihiro Itoh, Sakiko Maruyama, Mineko Kurotaki, Hidehiko Nakagawa, Naoki Miyata: Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor Bioorganic and Medicinal Chemistry Letters. 2007.03; 17 (6): 1558-1561. ( PubMed , DOI )

  1. Takayoshi Suzuki, Akiyasu Kouketsu, Yukihiro Itoh, Shinya Hisakawa, Satoko Maeda, Minoru Yoshida, Hidehiko Nakagawa, Naoki Miyata: Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate Journal of Medicinal Chemistry. 2006.08; 49 (16): 4809-4812. ( PubMed , DOI )

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