1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
ACS Medicinal Chemistry Letters2014Vol. 5(11), pp. 1190–1195
Citations Over TimeTop 10% of 2014 papers
Emmanuel H. Demont, Paul Bamborough, Chun‐wa Chung, Peter D. Craggs, David J. Fallon, Laurie Gordon, Paola Grandi, Clare I. Hobbs, Jameed Hussain, Emma J. Jones, Armelle Le Gall, Anne‐Marie Michon, Darren J. Mitchell, Rab K. Prinjha, Andy D. Roberts, Robert J. Sheppard, Robert J. Watson
Abstract
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 structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.
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