- GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
ACS medicinal chemistry letters (2016-06-22)
Paul Bamborough, Heather A Barnett, Isabelle Becher, Mark J Bird, Chun-Wa Chung, Peter D Craggs, Emmanuel H Demont, Hawa Diallo, David J Fallon, Laurie J Gordon, Paola Grandi, Clare I Hobbs, Edward Hooper-Greenhill, Emma J Jones, Robert P Law, Armelle Le Gall, David Lugo, Anne-Marie Michon, Darren J Mitchell, Rab K Prinjha, Robert J Sheppard, Allan J B Watson, Robert J Watson
PMID27326325
RESUMEN
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.