Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 11, Pages 1190-1195Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml5002932
Keywords
BRPF1; BRPF2; BRD1; BRPF3; bromodomain; chemical probe; epigenetics; fragment; inhibitor
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The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structureactivity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.
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