期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 24, 页码 7950-7953出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm901543m
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资金
- Intramural NIH HHS [Z01 HG200319-05] Funding Source: Medline
- NIGMS NIH HHS [RC1 GM090732] Funding Source: Medline
SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as it potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the G9a-8 complex, the first cocrystal structure of G9a with a small molecule inhibitor, was obtained. The cocrystal structure validated our binding hypothesis and will enable structure-based design of novel inhibitors. 8 is a useful tool for investigating the biology of G9a and its roles in chromatin remodeling.
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