Clinical progress and pharmacology of small molecule bromodomain inhibitors

Natalie H Theodoulou, Nicholas CO Tomkinson, Rab K Prinjha, Philip G Humphreys

Research output: Contribution to journalArticlepeer-review

52 Citations (Scopus)
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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.
Original languageEnglish
Pages (from-to)58-66
Number of pages9
JournalCurrent Opinion in Chemical Biology
Early online date10 Jun 2016
Publication statusPublished - 31 Aug 2016


  • bromodomain inhibitors
  • epigenetic therapeutics
  • drug discovery
  • extra terminal
  • small molecule inhibitors
  • clinical assets
  • disease pathways


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