Advancements in the development of non-BET bromodomain chemical probes

Michael A. Clegg, Nicholas C. O. Tomkinson, Rab K. Prinjhal, Philip G. Humphreys

Research output: Contribution to journalReview article

6 Citations (Scopus)
48 Downloads (Pure)

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.
Original languageEnglish
Pages (from-to)362-385
Number of pages24
JournalChemMedChem
Volume14
Issue number4
Early online date9 Jan 2019
DOIs
Publication statusPublished - 19 Feb 2019

Keywords

  • acetylated lysines
  • chemical probes
  • epigenetics
  • non-BET bromodomains
  • target validation

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