| Project/Area Number |
26670052
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tokyo Medical and Dental University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
HIRANO Tomoya 東京医科歯科大学, 生体材料工学研究所, 准教授 (20396980)
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | ヒストンメチル化酵素 / 阻害剤 / 検出法 / 芳香族求核置換反応 / SET7/9 / シプロヘプタジン / スクリーニング / 蛍光法 / 結晶構造 / 酵素阻害剤 / リシン / N―メチルリシン / 構造活性相関 |
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| Outline of Final Research Achievements |
In this project, development of a novel method to detect histone methylation and of novel HMT inhibitors were examined.
1) Among aromatic electrophiles, we found that 1-fluoro-2,5-dinitrobenzene reacted with N-methyllysine faster than with lysine. By using this reagent, we developed novel detection method of N-methylation of lysine.
2) Novel SET7/9 inhibitors were developed by using cyproheptadine as a lead compound, that was identified as SET7/9 inhibitor by screening of our chemical library.
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