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ChemMedChem
Article . 2019 . Peer-reviewed
License: Wiley Online Library User Agreement
Data sources: Crossref
ChemMedChem
Article . 2019
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Advancements in the Development of non‐BET Bromodomain Chemical Probes

Authors: Michael A. Clegg; Nicholas C. O. Tomkinson; Rab K. Prinjha; Philip G. Humphreys;

Advancements in the Development of non‐BET Bromodomain Chemical Probes

Abstract

AbstractThe bromodomain and extra terminal (BET) family of bromodomain‐containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high‐quality chemical probes for their tandem bromodomains. In turn, these chemical probes have helped reveal the profound biological role of the BET bromodomains and their role in disease, ultimately leading to a number of molecules in active clinical development. However, the BET subfamily represents just 8/61 of the known human bromodomains, and attention has now expanded to the biological role of the remaining 53 non‐BET bromodomains. Rapid growth of this research area has been accompanied by a greater understanding of the requirements for an effective bromodomain chemical probe and has led to a number of new non‐BET bromodomain chemical probes being developed. Advances since December 2015 are discussed, highlighting the strengths/caveats of each molecule, and the value they add toward validating the non‐BET bromodomains as tractable therapeutic targets.

Keywords

610, Nuclear Proteins, Proteins, Antigens, Nuclear, Nerve Tissue Proteins, p300-CBP-Associated Factor, 540, DNA-Binding Proteins, Chemistry, Bromodomain Containing Proteins, Protein Domains, Molecular Probes, Humans, QD, p300-CBP Transcription Factors, Phylogeny, Adaptor Proteins, Signal Transducing, Transcription Factors

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    popularity
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    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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!
43
Top 10%
Top 10%
Top 10%
Green