2. Academic Validation
  3. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain

  • ACS Med Chem Lett. 2016 May 9;7(6):552-7. doi: 10.1021/acsmedchemlett.6b00092.
Paul Bamborough 1,  Heather A Barnett 1,  Isabelle Becher 2,  Mark J Bird 1,  Chun-Wa Chung 1,  Peter D Craggs 1,  Emmanuel H Demont 1,  Hawa Diallo 1,  David J Fallon 3,  Laurie J Gordon 1,  Paola Grandi 2,  Clare I Hobbs 1,  Edward Hooper-Greenhill 1,  Emma J Jones 1,  Robert P Law 3,  Armelle Le Gall 1,  David Lugo 1,  Anne-Marie Michon 2,  Darren J Mitchell 1,  Rab K Prinjha 1,  Robert J Sheppard 1,  Allan J B Watson 4,  Robert J Watson 1
Affiliations

Affiliations

  • 1 Epinova Discovery Performance Unit, Quantitative Pharmacology, Experimental Medicine Unit, Flexible Discovery Unit, and Platform Technology and Science, GlaxoSmithKline , Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.
  • 2 Cellzome GmbH, GlaxoSmithKline , Meyerhofstrasse 1, 69117 Heidelberg, Germany.
  • 3 Epinova Discovery Performance Unit, Quantitative Pharmacology, Experimental Medicine Unit, Flexible Discovery Unit, and Platform Technology and Science, GlaxoSmithKline, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, U.K.
  • 4 WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde , Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, U.K.
PMID: 27326325 DOI: 10.1021/acsmedchemlett.6b00092
Abstract

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.

Keywords

BET; BRD1; BRPF1; BRPF2; BRPF3; bromodomain; chemical probe; epigenetics; inhibitor.

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