Advancements in the development of non-BET bromodomain chemical probes

Clegg, Michael A. and Tomkinson, Nicholas C. O. and Prinjhal, Rab K. and Humphreys, Philip G. (2019) Advancements in the development of non-BET bromodomain chemical probes. ChemMedChem, 14 (4). pp. 362-385. ISSN 1860-7179 (https://doi.org/10.1002/cmdc.201800738)

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Abstract

The 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.

ORCID iDs

Clegg, Michael A., Tomkinson, Nicholas C. O. ORCID logoORCID: https://orcid.org/0000-0002-5509-0133, Prinjhal, Rab K. and Humphreys, Philip G.;
  • Item type:Article
    ID code:68690
    Dates:
    Date
    Event
    19 February 2019
    Published
    9 January 2019
    Published Online
    9 January 2019
    Accepted
    Notes:This is the peer reviewed version of the following article: Clegg, MA, Tomkinson, NCO, Prinjhal, RK & Humphreys, PG 2019, 'Advancements in the development of non-BET bromodomain chemical probes' ChemMedChem, vol. 14, no. 4, pp. 362-385, which has been published in final form at https://doi.org/10.1002/cmdc.201800738. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions.
    Subjects:Science > Chemistry
    Department:Faculty of Science > Pure and Applied Chemistry
    Depositing user: Pure Administrator
    Date deposited:02 Jul 2019 15:11
    Last modified:11 Nov 2024 12:21
    URI:https://strathprints.strath.ac.uk/id/eprint/68690
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