基本情報

写真a

伊藤　幸裕(イトウ　ユキヒロ)

ITOH Yukihiro


職名

教授
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取得学位 【 表示 ／ 非表示 】

  • 博士（薬学）  東京大学

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経歴(学内) 【 表示 ／ 非表示 】

  • 2025年06月
    -
    現在
    東京科学大学 教育研究組織 総合研究院 生材研・創薬科学研究部門 生命医薬化学分野 教授
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経歴(学外) 【 表示 ／ 非表示 】

  • 2019年04月
    -
    2020年05月
    京都府立医科大学 医学(系)研究科(研究院) 准教授
  • 2020年06月
    -
    2025年05月
    大阪大学 産業科学研究所 准教授
  • 2020年06月
    -
    現在
    京都府立医科大学 客員講師
  • 2025年06月
    -
    現在
    東京科学大学 総合研究院生体材料工学研究所 教授
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研究分野 【 表示 ／ 非表示 】

  • 薬系化学、創薬科学

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資格、免許 【 表示 ／ 非表示 】

  • 薬剤師

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研究テーマ 【 表示 ／ 非表示 】

  • エピジェネティクス複合体を標的としたキメラ分子の創製研究，2024年04月 - 2027年03月

  • 分子接着剤を用いた超効率的な組織再生誘導，2023年06月 - 2025年03月

  • クリックケミストリーに基づく生物活性化合物創製法の確立，2022年04月 - 2026年03月

  • 標的誘導型合成による革新的医薬品候補化合物の創製，2021年04月 - 2024年03月

  • RNA分解誘導化合物の開発とその薬学的応用，2020年07月 - 2023年03月

  • ユビキチン化タンパク質ならびにその連結様式を解析するためのケミカルプローブ創製，2019年04月 - 2021年03月

  • 人工ユビキチン化合物の創製とその応用，2017年04月 - 2020年03月

  • 酵素反応機構を基に設計したユビキチン活性化酵素阻害薬の創製，2014年04月 - 2017年03月

  • 触媒メカニズムに基づくヒストン脱メチル化酵素（ＬＳＤ１）阻害薬の創製，2012年08月 - 2014年03月

▼全件表示

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競争的資金等の研究課題 【 表示 ／ 非表示 】

  • クリックケミストリーに基づく生物活性化合物創製法の確立

    文部科学省/日本学術振興会 : 2023年 - 2025年

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論文・総説 【 表示 ／ 非表示 】

  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. ( 医中誌 )

  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. ( 医中誌 )

  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. ( 医中誌 )

  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. ( 医中誌 )

  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. ( 医中誌 )

  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. ( 医中誌 )

  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. ( 医中誌 )

  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 )

  41. 山下 泰信, 高田 悠里, 伊藤 幸裕, 鈴木 孝禎. HDAC8選択的阻害薬の創製とPROTACへの応用 MEDCHEM NEWS. 2023.11; 33 (4): 181-186. ( DOI )

  42. 伊藤 幸裕. 【分子標的薬を極める】分子標的薬のこれから　エピジェネティクス制御を作用機序とする分子標的薬 小児内科. 2023.02; 55 (2): 181-183. ( 医中誌 )

  43. 伊藤 幸裕. 速度論的概念に基づく酵素阻害薬の創製研究 上原記念生命科学財団研究報告集. 2019.12; 33 1-4. ( 医中誌 )

  44. Challenges of young chemists to be global 2019; 139 (2): 185-186. ( PubMed, DOI )

  45. 伊藤 幸裕, 鈴木 孝禎. 薬学における生命指向型化学(「薬」創りの新発想)　有機化学の力を借りた「薬」創り 薬学雑誌. 2017.03; 137 (3): 283-292. ( 医中誌 )

  46. 東條 敏史, 伊藤 幸裕, 展 鵬, 太田 庸介, 鈴木 美紀, 内田 周作, 鈴木 孝禎. Click Chemistryを用いたHDAC1/2選択的阻害薬の創製 日本薬学会年会要旨集. 2016.03; 136年会 (2): 125. ( 医中誌 )

  47. 塚本 修一朗, 榮 慶丈, 伊藤 幸裕, 鈴木 孝禎, 岡本 祐幸. 22aPS-113 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エピジェネティックな酵素の阻害剤の選択性に関する研究 日本物理学会講演概要集. 2016; 71 3323. ( DOI )

  48. 伊藤 幸裕, 鈴木 孝禎. エピジェネティクスを操る小分子化合物 ファルマシア. 2014; 50 (11): 1107-1111. ( DOI )

  49. 石川 稔, 伊藤 幸裕, 内藤 幹彦, 橋本 祐一. 2-II-24 細胞内レチノイド結合タンパク質の分解を誘導するレチノイン酸連結化合物の創製(一般演題,日本ビタミン学会第62回大会発表要旨) ビタミン. 2010.04; 84 (4): 189.

  50. 伊藤 幸裕, 鈴木 孝禎, 宮田 直樹. HDAC6選択的阻害薬--HDAC6選択的阻害薬の腫瘍細胞に対する効果 (第1土曜特集 がん分子標的治療の最先端) -- (低分子阻害剤) 医学のあゆみ. 2008.01; 224 (1): 71-74.

  51. Mukherjee, A; Yamashita, Y; Maeda, R; Akiyama, T; Endo, K; Takada, Y; Tsumoto, H; Moriyama, Y; Ito, A; Shirai, F; Tachibana, M; Itoh, Y; Suzuki, T. 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 )

  52. A Deep-Learning-Aided Drug Screening Based on Visualization of a Hidden Layer as Chemical Space 2025.06; ( DOI )

  53. Identification of Proteolysis Targeting Chimeras (PROTACs) for Lysine Demethylase 5 and Their Neurite Outgrowth-Promoting Activity 2024.07; 72 (7): 638-647. ( DOI )

  54. 伊藤幸裕, 高田悠里, 山下泰信, 鈴木孝禎. 創薬モダリティの高度化と次世代動物評価モデル 4.タンパク質間相互作用阻害を標的とした創薬モダリティ 実験医学. 2024; 42 (2):

  55. Discovery of Selective Histone Deacetylase 1 and 2 Inhibitors: Screening of a Focused Library Constructed by Click Chemistry, Kinetic Binding Analysis, and Biological Evaluation 2023.10; 66 (22): 15171-15188. ( PubMed, DOI )

  56. Medicinal Chemistry Research on Targeting Epigenetic Complexes 2022.07; 80 (7): 664-675. ( DOI )

  57. N<sup>+</sup>-C-H…O Hydrogen Bonds in Protein-Ligand Complexes and their Application to Drug Design 2020.12; 78 (12): 1151-1162. ( DOI )

  58. Metalloprotein-Catalyzed Click Reaction for In Situ Generation of a Potent Inhibitor 2020.04; 10 (10): 5383-5392. ( DOI )

  59. Okuhira K, Shoda T, Omura R, Ohoka N, Hattori T, Shibata N, Demizu Y, Sugihara R, Ichino A, Kawahara H, Itoh Y, Ishikawa M, Hashimoto Y, Kurihara M, Itoh S, Saito H, Naito M. Targeted Degradation of Proteins Localized in Subcellular Compartments by Hybrid Small Molecules. Molecular pharmacology. 2017.03; 91 (3): 159-166. ( PubMed, DOI )

  60. Itoh Y, Suzuki T. "Drug" Discovery with the Help of Organic Chemistry. Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan. 2017; 137 (3): 283-292. ( PubMed, DOI )

  61. Chemical biology for pharmaceutical sciences (novel ideas for “drug” discovery) 2017; 137 (3): 281-282. ( PubMed, DOI )

  62. Mellini P, Itoh Y, Tsumoto H, Li Y, Suzuki M, Tokuda N, Kakizawa T, Miura Y, Takeuchi J, Lahtela-Kakkonen M, Suzuki T. Potent mechanism-based sirtuin-2-selective inhibition by an <i>in situ</i>-generated occupant of the substrate-binding site, "selectivity pocket" and NAD<sup>+</sup>-binding site. Chemical science. 2017; 8 (9): 6400-6408. ( PubMed, DOI )

  63. Higuchi F, Uchida S, Yamagata H, Abe-Higuchi N, Hobara T, Hara K, Kobayashi A, Shintaku T, Itoh Y, Suzuki T, Watanabe Y. Hippocampal MicroRNA-124 Enhances Chronic Stress Resilience in Mice. The Journal of neuroscience : the official journal of the Society for Neuroscience. 2016.07; 36 (27): 7253-7267. ( PubMed, DOI )

  64. Kakizawa T, Mizukami T, Itoh Y, Hasegawa M, Sasaki R, Suzuki T. Evaluation of phenylcyclopropylamine compounds by enzymatic assay of lysine-specific demethylase 2 in the presence of NPAC peptide. Bioorganic & medicinal chemistry letters. 2016.02; 26 (4): 1193-1195. ( PubMed, DOI )

  65. Itoh Y, Aihara K, Mellini P, Tojo T, Ota Y, Tsumoto H, Solomon VR, Zhan P, Suzuki M, Ogasawara D, Shigenaga A, Inokuma T, Nakagawa H, Miyata N, Mizukami T, Otaka A, Suzuki T. Identification of SNAIL1 Peptide-Based Irreversible Lysine-Specific Demethylase 1-Selective Inactivators. Journal of medicinal chemistry. 2016.02; 59 (4): 1531-1544. ( PubMed, DOI )

  66. Miyamura S, Araki M, Ota Y, Itoh Y, Yasuda S, Masuda M, Taniguchi T, Sowa Y, Sakai T, Suzuki T, Itami K, Yamaguchi J. C-H activation enables a rapid structure-activity relationship study of arylcyclopropyl amines for potent and selective LSD1 inhibitors. Organic & biomolecular chemistry. 2016; 14 (36): 8576-8585. ( PubMed, DOI )

  67. Itoh Y, Suzuki M, Matsui T, Ota Y, Hui Z, Tsubaki K, Suzuki T. False HDAC Inhibition by Aurone Compound. Chemical & pharmaceutical bulletin. 2016; 64 (8): 1124-1128. ( PubMed, DOI )

  68. Molecular technology for controlling epigenetics: Regulation of histone acetylation and methylation by small molecules 2016; 74 (5): 441-452. ( DOI )

  69. 伊藤幸裕, 粟飯原圭佑, MELLINI Paolo, 東條敏史, 太田庸介, 津元裕樹, SOLOMON Viswas Raja, ZHAN Peng, 鈴木美紀, 小笠原大介, 重永章, 猪熊翼, 中川秀彦, 宮田直樹, 水上民夫, 大高章, 鈴木孝禎. ヒドラジン構造を持つペプチド性LSD1阻害薬の創製 メディシナルケミストリーシンポジウム講演要旨集. 2016; 34th

  70. Ota Y, Itoh Y, Kaise A, Ohta K, Endo Y, Masuda M, Sowa Y, Sakai T, Suzuki T. Targeting Cancer with PCPA-Drug Conjugates: LSD1 Inhibition-Triggered Release of 4-Hydroxytamoxifen. Angewandte Chemie (International ed. in English). 2016; 55 (52): 16115-16118. ( PubMed, DOI )

  71. Itoh Y, Sawada H, Suzuki M, Tojo T, Sasaki R, Hasegawa M, Mizukami T, Suzuki T. 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 )

  72. Kakizawa T, Ota Y, Itoh Y, Tsumoto H, Suzuki T. Histone H3 peptide based LSD1-selective inhibitors. Bioorganic & medicinal chemistry letters. 2015.05; 25 (9): 1925-1928. ( PubMed, DOI )

  73. Design, synthesis, and biological activity of N-alkylated analogue of NCL1, a selective inhibitor of lysine-specific demethylase 1 2015.03; 6 (3): 407-412. ( DOI )

  74. Zhan P, Song Y, Itoh Y, Suzuki T, Liu X. Recent advances in the structure-based rational design of TNKSIs. Molecular bioSystems. 2014.11; 10 (11): 2783-2799. ( PubMed, DOI )

  75. Sekizawa H, Amaike K, Itoh Y, Suzuki T, Itami K, Yamaguchi J. 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 )

  76. Tatum PR, Sawada H, Ota Y, Itoh Y, Zhan P, Ieda N, Nakagawa H, Miyata N, Suzuki T. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorganic & medicinal chemistry letters. 2014.04; 24 (8): 1871-1874. ( PubMed, DOI )

  77. Suzuki T, Muto N, Bando M, Itoh Y, Masaki A, Ri M, Ota Y, Nakagawa H, Iida S, Shirahige K, Miyata N. Design, synthesis, and biological activity of NCC149 derivatives as histone deacetylase 8-selective inhibitors. ChemMedChem. 2014.03; 9 (3): 657-664. ( PubMed, DOI )

  78. Itoh Y, Ogasawara D, Ota Y, Mizukami T, Suzuki T. 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 )

  79. Target-guided synthesis: Medicinal chemistry strategy to allow target enzymes themselves to synthesize their own inhibitors 2014; 72 (6): 702-716. ( DOI )

  80. Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N. 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 )

  81. Matsuya Y, Kobayashi Y, Uchida S, Itoh Y, Sawada H, Suzuki T, Miyata N, Sugimoto K, Toyooka N. Search for a novel SIRT1 activator: structural modification of SRT1720 and biological evaluation. Bioorganic & medicinal chemistry letters. 2013.09; 23 (17): 4907-4910. ( PubMed, DOI )

  82. Ogasawara D, Itoh Y, Tsumoto H, Kakizawa T, Mino K, Fukuhara K, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N, Suzuki T. Lysine-specific demethylase 1-selective inactivators: protein-targeted drug delivery mechanism. Angewandte Chemie (International ed. in English). 2013.08; 52 (33): 8620-8624. ( PubMed, DOI )

  83. Suzuki T, Kasuya Y, Itoh Y, Ota Y, Zhan P, Asamitsu K, Nakagawa H, Okamoto T, Miyata N. 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 )

  84. Itoh Y, Suzuki T, Miyata N. Small-molecular modulators of cancer-associated epigenetic mechanisms. Molecular bioSystems. 2013.05; 9 (5): 873-896. ( PubMed, DOI )

  85. Suzuki T, Ota Y, Ri M, Bando M, Gotoh A, Itoh Y, Tsumoto H, Tatum PR, Mizukami T, Nakagawa H, Iida S, Ueda R, Shirahige K, Miyata N. 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 )

  86. Itoh Y, Ishikawa M, Kitaguchi R, Okuhira K, Naito M, Hashimoto Y. Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist. Bioorganic & medicinal chemistry letters. 2012.07; 22 (13): 4453-4457. ( PubMed, DOI )

  87. Suzuki T, Khan MN, Sawada H, Imai E, Itoh Y, Yamatsuta K, Tokuda N, Takeuchi J, Seko T, Nakagawa H, Miyata N. 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 )

  88. Itoh Y, Kitaguchi R, Ishikawa M, Naito M, Hashimoto Y. Design, synthesis and biological evaluation of nuclear receptor-degradation inducers. Bioorganic & medicinal chemistry. 2011.11; 19 (22): 6768-6778. ( PubMed, DOI )

  89. Itoh Y, Ishikawa M, Kitaguchi R, Sato S, Naito M, Hashimoto Y. Development of target protein-selective degradation inducer for protein knockdown. Bioorganic & medicinal chemistry. 2011.05; 19 (10): 3229-3241. ( PubMed, DOI )

  90. Okuhira K, Ohoka N, Sai K, Nishimaki-Mogami T, Itoh Y, Ishikawa M, Hashimoto Y, Naito M. 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 )

  91. Hamada S, Suzuki T, Mino K, Koseki K, Oehme F, Flamme I, Ozasa H, Itoh Y, Ogasawara D, Komaarashi H, Kato A, Tsumoto H, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N. 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 )

  92. Itoh Y, Ishikawa M, Naito M, Hashimoto Y. 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 )

  93. 浜田翔平, 鈴木孝禎, 鈴木孝禎, 伊藤幸裕, 三野光識, 津元裕樹, 中川秀彦, 水上民夫, 宮田直樹. Jumonji Cドメインを含むヒストン脱メチル化酵素阻害薬の創製 日本薬学会年会要旨集. 2010; 130th (2):

  94. Hamada S, Kim TD, Suzuki T, Itoh Y, Tsumoto H, Nakagawa H, Janknecht R, Miyata N. Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors. Bioorganic & medicinal chemistry letters. 2009.05; 19 (10): 2852-2855. ( PubMed, DOI )

  95. 浜田翔平, 鈴木孝禎, 伊藤幸裕, 三野光識, 津元裕樹, 中川秀彦, 水上民夫, 宮田直樹. N-oxalylglycine誘導体の合成及びヒストン脱メチル化酵素JMJD2阻害活性評価 メディシナルケミストリーシンポジウム講演要旨集. 2009; 28th

  96. Suzuki T, Igari S, Hirasawa A, Hata M, Ishiguro M, Fujieda H, Itoh Y, Hirano T, Nakagawa H, Ogura M, Makishima M, Tsujimoto G, Miyata N. Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists. Journal of medicinal chemistry. 2008.12; 51 (23): 7640-7644. ( PubMed, DOI )

  97. Itoh Y, Suzuki T, Miyata N. Isoform-selective histone deacetylase inhibitors. Current pharmaceutical design. 2008.02; 14 (6): 529-544. ( PubMed, DOI )

  98. Itoh Y, Suzuki T, Kouketsu A, Suzuki N, Maeda S, Yoshida M, Nakagawa H, Miyata N. 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 )

  99. Suzuki T, Hisakawa S, Itoh Y, Suzuki N, Takahashi K, Kawahata M, Yamaguchi K, Nakagawa H, Miyata N. Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors. Bioorganic & medicinal chemistry letters. 2007.08; 17 (15): 4208-4212. ( PubMed, DOI )

  100. Suzuki T, Hisakawa S, Itoh Y, Maruyama S, Kurotaki M, Nakagawa H, Miyata N. Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor. Bioorganic & medicinal chemistry letters. 2007.03; 17 (6): 1558-1561. ( PubMed, DOI )

  101. Suzuki T, Kouketsu A, Itoh Y, Hisakawa S, Maeda S, Yoshida M, Nakagawa H, Miyata N. 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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  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

  7. 椎村 祐樹, 伊藤 幸裕, イム・ドヒョン , 岡田 咲良, 岩田 想, 鈴木 孝禎, 佐藤 貴弘. グレリン受容体を標的とした低分子化合物創製の試み. 日本内分泌学会雑誌 2025.05.01

  8. 花谷 優太朗, 黒原 崇, 山下 泰信, 高田 悠里, 伊藤 幸裕, 鈴木 孝禎. RNA創薬を志向した金属錯体型RNA分解分子の開発. 日本薬学会年会要旨集 2022.03.01

  9. 荻原 洲介, 小松 徹, 伊藤 幸裕, 三宅 由花, 鈴木 孝禎, 小島 宏建, 岡部 隆義, 長野 哲雄, 浦野 泰照. 有機小分子蛍光プローブを用いた高感度S-adenosylmethionine(SAM)検出系の開発とPathway-Oriented Screeningへの応用. 日本薬学会年会要旨集 2021.03.01

  10. 萩原 洲介, 小松 徹, 伊藤 幸裕, 三宅 由花, 鈴木 孝禎, 小島 宏建, 岡部 隆義, 長野 哲雄, 浦野 泰照. 有機小分子蛍光プローブを用いた高感度S-adenosylmethionine(SAM)の検出系の開発とスクリーニングへの応用. 日本生化学会大会プログラム・講演要旨集 2019.09.01

  11. Jaikhan Pattaporn, 伊藤 幸裕, 鈴木 孝禎. エピジェネティクス研究最前線　基礎から創薬応用まで多角的に捉える　ヒストン脱アセチル化酵素3阻害薬およびヒストン脱メチル化酵素阻害薬の創製. 日本薬学会年会要旨集 2019.03.01

  12. 伊藤 幸裕. 合理的な分子設計と独特な創薬方法論が導くリシン修飾酵素制御化合物の創製. 日本薬学会年会要旨集 2019.03.01

  13. 伊藤 幸裕, 鈴木 孝禎. 創薬化学への応用を志向したN+-C-H...O水素結合の計算化学的解析. 日本薬学会年会要旨集 2017.03.01

  14. 東條 敏史, 伊藤 幸裕, 李 頴, Van Der Wiel Alexander, 鈴木 孝禎. 速度論的HDAC2選択性を示す阻害薬の創製. 日本薬学会年会要旨集 2017.03.01

  15. 太田 庸介, 伊藤 幸裕, 鈴木 孝禎. 多分野連携で織り成すこれからの医療　アンメットメディカルニーズの充足を目指して　リシン特異的脱メチル化酵素LSD1を標的とした創薬研究. 日本薬学会年会要旨集 2017.03.01

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