2016 Fiscal Year Final Research Report
Development of novel detection method for histone methylation and HMT inhibitors
| Project/Area Number |
26670052
|
|---|
| Research Category |
Grant-in-Aid for Challenging Exploratory Research
|
| Allocation Type | Multi-year Fund |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Tokyo Medical and Dental University |
|---|
Principal Investigator |
|
|---|
| 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)
|
|---|
| Project Period (FY) |
2014-04-01 – 2017-03-31
|
| 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 |
|---|
| 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.
|
| Free Research Field |
医薬化学
|
