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

Emmanuel H. Demont | Zendy; Paul Bamborough | Zendy; Chunwa Chung | Zendy; Peter D. Craggs | Zendy; David J. Fallon | Zendy; Laurie Gordon | Zendy; Paola Grandi | Zendy; Clare I. Hobbs | Zendy; Jameed Hussain | Zendy; Emma J. Jones | Zendy; Armelle Le Gall | Zendy; AnneMarie Michon | Zendy; Darren J. Mitchell | Zendy; Rab K. Prinjha | Zendy; Andy D. Roberts | Zendy; Robert J. Sheppard | Zendy; Robert J. Watson | Zendy

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

Author(s) -

Emmanuel H. Demont,

Paul Bamborough,

Chunwa Chung,

Peter D. Craggs,

David J. Fallon,

Laurie Gordon,

Paola Grandi,

Clare I. Hobbs,

Jameed Hussain,

Emma J. Jones,

Armelle Le Gall,

AnneMarie Michon,

Darren J. Mitchell,

Rab K. Prinjha,

Andy D. Roberts,

Robert J. Sheppard,

Robert J. Watson

Publication year - 2014

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml5002932

Subject(s) - bromodomain , chemistry , pharmacology , medicine , biochemistry , epigenetics , gene

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.

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