Development of novel detection method for histone methylation and HMT inhibitors
| 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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Report
(4 results)
Research Products
(21 results)
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[Journal Article] Identification of cyproheptadine as an inhibitor of SET domain containing lysine methyltransferase 7/9 (Set7/9) that regulates estrogen-dependent transcription.2016
Author(s)
Takemoto Y, Ito A, Niwa H, Okamura M, Fujiwara T, Hirano T, Handa N, Umehara T, Sonoda T, Ogawa K, Tariq M, Nishino N, Dan S, Kagechika H, Yamori T, Yokoyama S, Yoshida M.
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Journal Title
J. Med. Chem.
Volume: 59
Issue: 8
Pages: 3650-3660
DOI
Related Report
Peer Reviewed / Acknowledgement Compliant
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[Journal Article] A new cell-based assay to evaluate myogenesis in mouse myoblast C2C12 cells2015
Author(s)
Kodaka, M.; Yang, Z.; Nakagawa, K.; Maruyama, J.; Xu, X.; Sarkar, A.; Ichimura, A.; Nasu, Y.; Ozawa, T.; Iwasa, H.; Ishigami-Yuasa, M.; Ito, S.; Kagechika, H.; Hata, Y.
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Journal Title
Exp. Cell. Res.
Volume: 336
Issue: 2
Pages: 171-181
DOI
Related Report
Peer Reviewed
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