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 journalArticle

45 Citations (Scopus)

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.
LanguageEnglish
Pages58-66
Number of pages9
JournalCurrent Opinion in Chemical Biology
Volume33
Early online date10 Jun 2016
DOIs
Publication statusPublished - 31 Aug 2016

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Clinical Pharmacology
Drug Discovery
Nervous System Diseases
Embryonic Development
Inflammation
Molecules
Research
Neoplasms

Keywords

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

Cite this

Theodoulou, Natalie H ; Tomkinson, Nicholas CO ; Prinjha, Rab K ; Humphreys, Philip G. / Clinical progress and pharmacology of small molecule bromodomain inhibitors. In: Current Opinion in Chemical Biology. 2016 ; Vol. 33. pp. 58-66.
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Clinical progress and pharmacology of small molecule bromodomain inhibitors. / Theodoulou, Natalie H; Tomkinson, Nicholas CO; Prinjha, Rab K ; Humphreys, Philip G.

In: Current Opinion in Chemical Biology, Vol. 33, 31.08.2016, p. 58-66.

Research output: Contribution to journalArticle

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