title: 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors 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. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the first potent, selective series of inhibitors of the BRPF1 bromodomain.
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Emmanuel H
authors.initials: EH
authors.lastname: Demont
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Paul
authors.initials: P
authors.lastname: Bamborough
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Chun-Wa
authors.initials: CW
authors.lastname: Chung
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Peter D
authors.initials: PD
authors.lastname: Craggs
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: David
authors.initials: D
authors.lastname: Fallon
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Laurie J
authors.initials: LJ
authors.lastname: Gordon
authors.affiliation: Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, 69117 Heidelberg, Germany.
authors.forename: Paola
authors.initials: P
authors.lastname: Grandi
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Clare I
authors.initials: CI
authors.lastname: Hobbs
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Jameed
authors.initials: J
authors.lastname: Hussain
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Emma J
authors.initials: EJ
authors.lastname: Jones
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Armelle
authors.initials: A
authors.lastname: Le Gall
authors.affiliation: Cellzome GmbH, Molecular Discovery Research, GlaxoSmithKline , Meyerhofstrasse 1, 69117 Heidelberg, Germany.
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Michon
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Darren J
authors.initials: DJ
authors.lastname: Mitchell
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Rab K
authors.initials: RK
authors.lastname: Prinjha
authors.affiliation: DMPK, GlaxoSmithKline , Park Road, Ware SG12 0DP, U.K.
authors.forename: Andy D
authors.initials: AD
authors.lastname: Roberts
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Sheppard
authors.affiliation: Epinova Discovery Performance Unit and Molecular Discovery Research, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Watson
keywords: BRD1; BRPF1; BRPF2; BRPF3; bromodomain; chemical probe; epigenetics; fragment; inhibitor