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1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain

DOI: 10.1021/ml5002932 DOI Help
PMID: 25408830 PMID Help

Authors: Emmanuel H. Demont (GlaxoSmithKline) , Paul Bamborough (GlaxoSmithKline) , Chun-wa Chung (GlaxoSmithKline) , Peter D. Craggs (GlaxoSmithKline) , David Fallon (GlaxoSmithKline) , Laurie J. Gordon (GlaxoSmithKline) , Paola Grandi (GlaxoSmithKline) , Clare I. Hobbs (GlaxoSmithKline) , Jameed Hussain (GlaxoSmithKline) , Emma J. Jones (GlaxoSmithKline) , Armelle Le Gall (GlaxoSmithKline) , Anne-marie Michon (GlaxoSmithKline) , Darren J. Mitchell (GlaxoSmithKline) , Rab K. Prinjha (GlaxoSmithKline) , Andy D. Roberts (GlaxoSmithKline) , Robert J. Sheppard (GlaxoSmithKline) , Robert J. Watson (GlaxoSmithKline)
Co-authored by industrial partner: Yes

Type: Journal Paper
Journal: Acs Medicinal Chemistry Letters , VOL 5 (11) , PAGES 1190 - 1195

State: Published (Approved)
Published: November 2014

Open Access Open Access

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.

Journal Keywords: Brpf1; Brpf2; Brd1; Brpf3; Bromodomain; Chemical Probe; Epigenetics; Fragment; Inhibitor

Subject Areas: Biology and Bio-materials


Instruments: I03-Macromolecular Crystallography