2020 Fiscal Year Final Research Report
Development of inhibitors that stablize the transition state of enzymatic reactions
| Project/Area Number |
16KT0060
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Multi-year Fund |
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| Section | 特設分野 |
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| Research Field |
Transition State Control
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| Research Institution | Osaka University (2019-2020)
Kyoto Prefectural University of Medicine (2016-2018) |
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Principal Investigator |
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| Project Period (FY) |
2016-07-19 – 2021-03-31
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| Keywords | 遷移状態 / 酵素 / 阻害薬 |
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| Outline of Final Research Achievements |
We have identifed isozyme-selective KDAC inhibitors that stablize the transition state of enzymatic reactions by the construction of a 2-aminoanilide compound library, kinetic screening and isozyme selectivity evaluation of the hit compounds. These inhibitors showed potent pharmacological effects such as memory-enhancing activity.
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| Free Research Field |
創薬化学
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| Academic Significance and Societal Importance of the Research Achievements |
超高齢化社会を迎えた日本では、がんやアルツハイマー病など、未だ特効薬の無い疾患が多数存在する。本研究により、酵素反応の遷移状態構造を考慮することにより、将来の医薬品につながる阻害剤の創製が可能であることが示された。本研究の成果は、アンメットメディカルニーズの高い疾患の治療につながることが期待される。
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