Clinical progress and pharmacology of small molecule bromodomain inhibitors

Theodoulou, Natalie H and Tomkinson, Nicholas CO and Prinjha, Rab K and Humphreys, Philip G (2016) Clinical progress and pharmacology of small molecule bromodomain inhibitors. Current Opinion in Chemical Biology, 33. pp. 58-66. ISSN 1367-5931

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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.