Clinical progress and pharmacology of small molecule bromodomain inhibitors

Curr Opin Chem Biol. 2016 Aug:33:58-66. doi: 10.1016/j.cbpa.2016.05.028. Epub 2016 Jun 10.

Abstract

Bromodomains have emerged as an exciting target class for drug discovery over the past decade. Research has primarily focused on the bromodomain and extra terminal (BET) family of bromodomains, which has led to the development of multiple small molecule inhibitors and an increasing number of clinical assets. The excitement centred on the clinical potential of BET inhibition has stimulated intense interest in the broader family and the growing number of non-BET bromodomain chemical probes has facilitated phenotypic investigations, implicating these targets in a variety of disease pathways including cancer, inflammation, embryonic development and neurological disorders.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Clinical Trials as Topic
  • Drug Discovery
  • Humans
  • Models, Molecular
  • Molecular Probes
  • Proteins / chemistry*
  • Small Molecule Libraries / chemistry*

Substances

  • Molecular Probes
  • Proteins
  • Small Molecule Libraries