Development of inhibitors that stablize the transition state of enzymatic reactions

2020 Fiscal Year Annual Research Report

• Project/Area Number: 16KT0060
• Research Institution: Osaka University
• Principal Investigator: 鈴木 孝禎 大阪大学, 産業科学研究所, 教授 (90372838)
• Project Period (FY): 2016-07-19 – 2021-03-31
• Keywords: 遷移状態 / 酵素 / 阻害薬

Outline of Annual Research Achievements

令和２年度は、前年度までに見出したKDACアイソザイムに対し、遷移状態構造を時間依存的に安定化する阻害薬の誘導体を設計、合成し、時間依存的なKDACアイソザイム阻害活性評価を行った。その結果、さらなる選択性を示す活性の高い時間依存的なKDACアイソザイム阻害薬を見出すことに成功した。

Research Products

• [Int'l Joint Research] Nirma University(インド)
  • Country Name: INDIA
  • Counterpart Institution: Nirma University
• [Journal Article] Discovery of novel tetrahydrobenzo[b]thiophene-3-carbonitriles as histone deacetylase inhibitors (2021)
  • Author(s): Gediya Piyush、Vyas Vivek K.、Carafa Vincenzo、Sitwala Nikum、Della Torre Laura、Poziello Angelita、Kurohara Takashi、Suzuki Takayoshi、Sanna Vinod、Raguraman Varalakshmi、Suthindhiran K.、Ghosh Debarpan、Bhatia Dhiraj、Altucci Lucia、Ghate Manjunath D.
  • Journal Title: Bioorganic Chemistry Volume: 110 Pages: 104801～104801
  • DOI: 10.1016/j.bioorg.2021.104801
  • Peer Reviewed / Int'l Joint Research
• [Journal Article] Downregulation of the Ca2+-activated K+ channel KCa3.1 in mouse preosteoblast cells treated with vitamin D receptor agonist (2020)
  • Author(s): Kito Hiroaki、Morihiro Haruka、Sakakibara Yuka、Endo Kyoko、Kajikuri Junko、Suzuki Takayoshi、Ohya Susumu
  • Journal Title: American Journal of Physiology-Cell Physiology Volume: 319 Pages: C345～C358
  • DOI: 10.1152/ajpcell.00587.2019
  • Peer Reviewed
• [Presentation] Identification of Epigenetic Inhibitors by Target-Guided Synthesis (2020)
  • Author(s): Takayoshi Suzuki
  • Organizer: Academia Sinica-Osaka University Symposium 2020
  • Int'l Joint Research / Invited
• [Remarks] 大阪大学産業科学研究所複合分子化学研究分野ホームページ
  • URL: https://www.sanken.osaka-u.ac.jp/labs/cmc/