Progress in the development of non-​BET bromodomain chemical probes

Theodoulou, Natalie H. and Tomkinson, Nicholas C. O. and Prinjha, Rab K. and Humphreys, Philip G. (2016) Progress in the development of non-​BET bromodomain chemical probes. ChemMedChem, 11 (5). pp. 477-487. ISSN 1860-7179 (

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The bromodomain and extra terminal (BET) family of bromodomains have been the focus of extensive research, leading to the development of many potent, selective chem. probes and recent clinical assets. The profound biol. 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 chem. probes for non-​BET bromodomains will facilitate elucidation of their precise biol. roles and potentially lead to the development of new medicines. This review summarises the progress made towards the development of non-​BET bromodomain chem. probes to date. In addn., we highlight the potential for future work in this new and exciting area.


Theodoulou, Natalie H., Tomkinson, Nicholas C. O. ORCID logoORCID:, Prinjha, Rab K. and Humphreys, Philip G.;