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ChemMedChem
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ChemMedChem
Article . 2016 . Peer-reviewed
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ChemMedChem
Article . 2016
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Progress in the Development of non‐BET Bromodomain Chemical Probes

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

Progress in the Development of non‐BET Bromodomain Chemical Probes

Abstract

AbstractThe 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.

Keywords

610, 540, Bromine, Crystallography, X-Ray, Chemistry, Molecular Probes, Animals, Humans, QD, Phylogeny

  • BIP!
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    citations
    The total number of citations received by all articles of the researcher of interest.
    40
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
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citations
The total number of citations received by all articles of the researcher of interest.
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
40
Top 10%
Top 10%
Top 10%
Green
bronze
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