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BET inhibitors: an updated patent review (2018-2021)

Huanhuan Chen1, Zhenling Liu1, Lili Zheng1

  • 1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, P. R. China.

Expert Opinion on Therapeutic Patents
|August 18, 2022
PubMed
Abstract

Insights

Bromodomain and extraterminal (BET) inhibitors show promise for treating cancer and other diseases by targeting gene transcription. Recent advancements reveal diverse BET inhibitor structures and dual-targeting strategies, indicating potential for next-generation therapies.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Bromodomain and extraterminal (BET) proteins are epigenetic readers regulating gene transcription and cell growth.
  • Dysregulation of BET proteins is implicated in cancer, inflammation, and metabolic diseases.
  • BET protein blockade is a promising therapeutic strategy, particularly for cancer treatment.

Purpose of the Study:

  • To review the molecular mechanisms of BET inhibitors.
  • To highlight research advancements in BET inhibitor patent literature from 2018-2021.
  • To discuss the therapeutic potential and future directions of BET inhibitors.

Main Methods:

  • Literature and patent searches were conducted using Web of Science, PubMed, SciFinder, WIPO, EPO, USPTO, and CNIPA databases.
  • Focus on patent literature published between 2018 and 2021.
  • Analysis of molecular mechanisms and structural diversity of identified BET inhibitors.

Main Results:

  • Identification of structurally diverse BET inhibitors, including pan-BET, selective (BD1/BD2), bivalent, dual kinase-BET inhibitors, and BET-PROTACs.
  • Significant progress in the discovery and development of potent and specific BET inhibitors.
  • Many BET inhibitors have advanced into clinical trials.

Conclusions:

  • BET inhibitors represent a promising class of therapeutics for various diseases, especially cancer.
  • Despite challenges, the development of next-generation BET inhibitors holds significant promise.
  • Continued research into BET inhibitor mechanisms and structures is crucial for advancing therapeutic applications.
Keywords:
BET inhibitorcancer therapypatentsmall molecule

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