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1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain
DOI:
10.1021/ml5002932
PMID:
25408830
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
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