Personnel Information

写真a

ITOH Yukihiro


Job title

Professor
To the head of this page.▲

Campus Career 【 display / non-display 】

  • 2025.06
    -
    Now
    Institute of Science Tokyo， -， Institute of Integrated Research， Division of Drug Discovery Science， -， Professor
To the head of this page.▲

External Career 【 display / non-display 】

  • 2019.04
    -
    2020.05
    Kyoto Prefectural University of Medicine, Associate Professor
  • 2020.06
    -
    2025.05
    Osaka University, The Institute of Scientific and Industrial Research, Associate Professor
  • 2020.06
    -
    Now
    Kyoto Prefectural University of Medicine,
  • 2025.06
    -
    Now
    Institute of Science Tokyo, Laboratory for Biomaterials and Bioengineering, Institute of Integrated Research, Professor
To the head of this page.▲

Research Areas 【 display / non-display 】

  • Pharmaceutical chemistry and drug development sciences

To the head of this page.▲

Qualification Acquired 【 display / non-display 】

  • Pharmacist

To the head of this page.▲
 

Research Theme 【 display / non-display 】

  • Development of chimera molecules targeting epigenetic complexes, 2024.04 - 2027.03

  • Development of innovative drug candidates by target guided synthesis, 2021.04 - 2024.03

  • Identification of artificial ubiquitin compounds and their application study, 2017.04 - 2020.03

  • Discovery of ubiquitin-activating enzyme inhibitors designed based on its catalytic mechanism, 2014.04 - 2017.03

  • Discovery of lysine-specific demethylase 1 Inhibitors based on enzymatic mechanism, 2012.08 - 2014.03

To the head of this page.▲

Published Papers & Misc 【 display / non-display 】

  1. 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 )

  2. 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 )

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

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

  5. 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 )

  6. 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 )

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

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

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

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

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

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

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

  14. 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 )

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

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

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

  18. 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 )

  19. 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 )

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

  21. 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 )

  22. 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 )

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

  24. 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 )

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

  26. 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<sup>+</sup>-Binding Site. Journal of medicinal chemistry. 2019.06; 62 (12): 5844-5862. ( PubMed, DOI )

  27. 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 )

  28. 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 )

  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. 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 )

  31. 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 )

  32. 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 )

  33. 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 )

  34. 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 )

  35. 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 )

  36. 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 )

  37. 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.

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

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

  40. 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 )

▼display all

To the head of this page.▲

Conference Activities & Talks 【 display / non-display 】

  1. Chotitumnavee Jiranan, Buranrat Benjaporn, Itoh Yukihiro, Suzuki Takayoshi. KDM5A阻害薬としてのα-ケトグルタル酸アナログのデザイン、合成および生物活性(Design, synthesis and biological activity of α-Ketoglutarate analogues as KDM5A inhibitors). 日本薬学会年会要旨集 2019.03.01

  2. ジャイカーン・パッタポーン , 伊藤 幸裕, 鈴木 孝禎. Histone lysine demethylase阻害物質としてのο-置換anilide化合物の同定(Identification of o-substituted anilide compounds as histone lysine demethylase inhibitors). 日本薬学会年会要旨集 2018.03.01

  3. Ota Yosuke, Itoh Yukihiro, Suzuki Takayoshi. LSD1阻害による抗癌剤の制御放出(Controlled Release of Anticancer Drugs by LSD1 Inhibition). 日本薬学会年会要旨集 2018.03.01

  4. Tsukamoto Shuichiro, Sakae Yoshitake, Itoh Yukihiro, Suzuki Takayoshi, Okamoto Yuko. 拡張アンサンブル分子動力学シミュレーションを用いたヒストン脱メチル化酵素阻害剤のアイソザイム選択制に関する研究(Study for Isozyme Selectivity of Lysine Demethylase Inhibitor by Using Generalized Ensemble Molecular Dynamics Simulations). 生物物理 2017.08.01

  5. Jaikhan Pattaporn, 伊藤 幸裕, 鈴木 孝禎. ヒストンリジン脱メチル化酵素阻害物質の探索のためのO-置換型アニリドライブラリの設計とスクリーニング(Design and Screening of an o-Substituted Anilide Library for Histone Lysine Demethylase Inhibitors). 日本薬学会年会要旨集 2017.03.01

  6. Mellini Paolo, 伊藤 幸裕, 津元 裕樹, 李 頴, 鈴木 美紀, 徳田 奈津子, 柿澤 多恵子, 三浦 ゆり, 竹内 淳, Lahtela-Kakkonen Maija, 鈴木 孝禎. 選択性ポケット、基質結合部位、およびNAD+-結合ポケットの部位の占有による分子機序を基盤としたSirtuin-2選択的なKPM-2の強力な阻害作用(Potent Mechanism-Based Sirtuin 2-Selective Inhibition by an in Situ Generated Occupant of Selectivity Pocket, Substrate-Binding Site, and NAD+-Bindig Pocket). 日本薬学会年会要旨集 2017.03.01

▼display all

To the head of this page.▲