Exploration of Chemical Reactions for Irreversible Protein Inhibition and Their Application to Drug Discovery

2021 Fiscal Year Final Research Report

• Project Area: Chemical Approaches for Miscellaneous / Crowding Live Systems
• Project/Area Number: 17H06349
• Research Category: Grant-in-Aid for Scientific Research on Innovative Areas (Research in a proposed research area)
• Allocation Type: Single-year Grants
• Review Section: Science and Engineering
• Research Institution: Kyushu University
• Principal Investigator: Ojida Akio 九州大学, 薬学研究院, 教授 (10343328)
• Co-Investigator(Kenkyū-buntansha): 小野 真弓 聖マリア学院大学, 看護学研究科, 教授 (80128347)
• Project Period (FY): 2017-06-30 – 2022-03-31
• Keywords: コバレントドラッグ / がん / 感染症 / ケミカルプロテオミクス

Outline of Final Research Achievements

In this research, we have developed medicinal-organic chemistry that aimed to develop new covalent drugs , which can specifically react with a target protein and inhibit its biological function under the miscellaneous biological conditions. we have focused on (1) development of covalent drugs with a CFA group targeting cancer and infectious diseases (2) finding new reactive groups suitable for selective covalent inhibition of proteins.

Free Research Field

ケミカルバイオロジー、創薬化学

Academic Significance and Societal Importance of the Research Achievements

本研究から得られる成果は、標的選択性の高いコバレントドラッグの分子デザインについての新しい知見を与え、副作用のない安全なコバレントドラッグの創薬開発に貢献できる可能性を有する。