GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.

ABSTRACT: The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies.

SUBMITTER: Bamborough P 

PROVIDER: S-EPMC4904261 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature