title: Progress in the Development of non-BET Bromodomain Chemical Probes.
abstract: The bromodomain and extra terminal (BET) family of bromodomains have been the focus of extensive research, leading to the development of many potent, selective chemical probes and recent clinical assets. The profound biology associated with BET bromodomain inhibition has provided a convincing rationale for targeting bromodomains for the treatment of disease. However, the BET family represents just eight of the at least 56 human bromodomains identified to date. Until recently, there has been significantly less interest in non-BET bromodomains, leaving a vast area of research and the majority of this new target class yet to be thoroughly investigated. It has been widely reported that several non-BET bromodomain containing proteins are associated with various diseases including cancer and HIV. Therefore, the development of chemical probes for non-BET bromodomains will facilitate elucidation of their precise biological roles and potentially lead to the development of new medicines. This review summarises the progress made towards the development of non-BET bromodomain chemical probes to date. In addition, we highlight the potential for future work in this new and exciting area.
authors.affiliation: 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.
authors.forename: Natalie H
authors.initials: NH
authors.lastname: Theodoulou
authors.affiliation: WestCHEM, Department of Pure and Applied Chemistry, Thomas Graham Building, University of Strathclyde, 295 Cathedral Street, Glasgow, G1 1XL, UK.
authors.forename: Nicholas C O
authors.initials: NC
authors.lastname: Tomkinson
authors.affiliation: Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire, SG1 2NY, UK.
authors.forename: Rab K
authors.initials: RK
authors.lastname: Prinjha
authors.affiliation: Epinova Epigenetics Discovery Performance Unit, GlaxoSmithKline R&D, Stevenage, Hertfordshire, SG1 2NY, UK. philip.g.humphreys@gsk.com.
authors.forename: Philip G
authors.identifier: http://orcid.org/0000-0002-8614-7155
authors.initials: PG
authors.lastname: Humphreys
mesh_terms: D000818:Animals; D001966:Bromine / Q000737:chemistry*; D018360:Crystallography, X-Ray; D006801:Humans; D015335:Molecular Probes; D010802:Phylogeny
chemical_list: D015335:Molecular Probes; D001966:Bromine
keywords: bromodomains; chemical probes; epigenetics; inhibitors; non-BET