Clinical progress and pharmacology of small molecule bromodomain inhibitors.
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.
Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, UK; WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, UK.
Natalie H
NH
Theodoulou
WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, UK.
Nicholas Co
NC
Tomkinson
Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, UK.
Rab K
RK
Prinjha
Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, UK. Electronic address: philip.g.humphreys@gsk.com.
Philip G
PG
Humphreys
D002986:Clinical Trials as Topic; D055808:Drug Discovery; D006801:Humans; D008958:Models, Molecular; D015335:Molecular Probes; D011506:Proteins / Q000737:chemistry*; D054852:Small Molecule Libraries / Q000737:chemistry*
D015335:Molecular Probes; D011506:Proteins; D054852:Small Molecule Libraries