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BET bromodomain inhibitors.

Martin P Schwalm1, Stefan Knapp2

  • 1Institut für Pharmazeutische Chemie, Goethe-University Frankfurt, Biozentrum, Max-von-Laue-Str. 9, 60438, Frankfurt Am Main, Germany; Structural Genomics Consortium, Goethe-University Frankfurt, Buchmann Institute for Life Sciences, Max-von-Laue-Str. 15, 60438, Frankfurt Am Main, Germany.

Current Opinion in Chemical Biology
|April 24, 2022
PubMed
Summary

Lysine acetylation regulates gene transcription via BET bromodomain proteins. New inhibitors allow deeper study of these epigenetic readers in diseases and clinical applications.

Keywords:
BETBRD4BromodomainJQ1PROTAC

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Area of Science:

  • Epigenetics and molecular biology, focusing on post-translational modifications and gene regulation.

Background:

  • Lysine acetylation serves as a crucial signal, creating binding sites for BET bromodomain proteins.
  • BET proteins are key regulators of lineage-specific gene transcription.

Purpose of the Study:

  • To review the advancements in understanding BET bromodomain proteins and their inhibitors.
  • To highlight the role of these proteins in disease mechanisms and therapeutic strategies.

Main Methods:

  • Utilizing potent and selective BET inhibitors for mechanistic studies in various disease models.
  • Analyzing the development of first-generation pan-BET inhibitors and second-generation selective inhibitors.

Main Results:

  • Availability of BET inhibitors has facilitated extensive research into their function.
  • Development of advanced inhibitors, including bifunctional and dual-targeting agents, has expanded research capabilities.

Conclusions:

  • BET bromodomain inhibitors are valuable tools for investigating acetylation-dependent transcription and BET-associated diseases.
  • These inhibitors show significant promise for further translational research and clinical applications in epigenetic therapies.