National Center for
4UYD: N-terminal Bromodomain Of Human Brd4 With 1,3-dimethyl-2- Oxo-2,3-dihydro-1h-1,3-benzodiazole-5-carboxamide
ACS Med Chem Lett (2014) 5 p.1190-1195
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.