期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 7, 期 2, 页码 162-166出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00380
关键词
Methyltransferase; PRMT5; property based optimization; structure guided design
资金
- Epizyme
- GlaxoSmithKline
The recent publication of a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) provides the scientific community with in vivo-active tool compound EPZ015666 (GSK3235025) to probe the underlying pharmacology of this key enzyme. Herein, we report the design and optimization strategies employed on an initial hit compound with poor in vitro clearance to yield in vivo tool compound EPZ015666 and an additional potent in vitro tool molecule EPZ015866 (GSK3203591).
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