2 research outputs found
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
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
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
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 <i>in vivo</i> studies