2. Academic Validation
  3. Chemical probes and inhibitors of bromodomains outside the BET family

Chemical probes and inhibitors of bromodomains outside the BET family

  • Medchemcomm. 2016 Dec 7;7(12):2246-2264. doi: 10.1039/c6md00373g.
Moses Moustakim 1 2 3,  Peter G K Clark 4,  Duncan A Hay 5,  Darren J Dixon 1,  Paul E Brennan 2 3
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Oxford, Oxford OX1 3TA, UK.
  • 2 Structural Genomics Consortium, University of Oxford, OX3 7DQ, UK. Email: paul.brennan@sgc.ox.ac.uk.
  • 3 Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, OX3 7FZ, UK.
  • 4 Department of Chemistry, Simon Fraser University, Burnaby V5A 1S6, Canada.
  • 5 Evotec (UK) Ltd, 114 Innovation Drive, Milton Park, Abingdon, Oxfordshire OX14 4RZ, UK.
PMID: 29170712 DOI: 10.1039/c6md00373g
Abstract

In the last five years, the development of inhibitors of bromodomains has emerged as an area of intensive worldwide research. Emerging evidence has implicated a number of non-BET bromodomains in the onset and progression of diseases such as Cancer, HIV Infection and inflammation. The development and use of small molecule chemical probes has been fundamental to pre-clinical evaluation of bromodomains as targets. Recent efforts are described highlighting the development of potent, selective and cell active non-BET bromodomain inhibitors and their therapeutic potential. Over half of typical bromodomains now have reported ligands, but those with atypical binding site residues remain resistant to chemical probe discovery efforts.

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