期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 8, 期 7, 页码 737-741出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.7b00132
关键词
Epigenetics; Bromodomain; CECR2; Probe
资金
- Argonne National Laboratory [DE-AC02-06CH11357]
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of cat eye syndrome chromosome region candidate 2 (CECR2). Screening of our internal medicinal chemistry collection led to the identification of a pyrrolopyridone chemical lead, and subsequent structure based drug design led to a potent and selective CECR2 bromodomain inhibitor (GNE-886) suitable for use as an in vitro tool compound.
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