BET Inhibitors as Anticancer Agents: A Patent Review

Imran Ali1, Gildon Choi1, Kwangho Lee1

  • 1Bio-Organic Science Division, Korea Research Institute of Chemical Technology, Daejeon 34114, Korea.

Abstract

Insights

Bromodomain and Extra Terminal (BET) inhibitors show promise as cancer therapeutics. This review covers BET inhibitor patent literature from 2010-2017, highlighting clinical development for various cancers.

Area of Science:

  • Epigenetics
  • Pharmacology
  • Oncology

Background:

  • Bromodomain and Extra Terminal (BET) proteins (BRD2, BRD3, BRD4, BRDT) are emerging cancer targets.
  • Small-molecule drug discovery is actively exploring BET proteins.

Purpose of the Study:

  • Review patent literature on BET inhibitors from 2010-2017.
  • Focus on cancer treatment and related diseases.

Main Methods:

  • BET proteins function as 'epigenetic readers' binding to acetylated histones.
  • Inhibition of BET proteins drives therapeutic applications and inhibitor development.

Main Results:

  • Significant patent activity from academia and industry on BET inhibitors.
  • Multiple BET inhibitors are in clinical development for diverse cancers.

Conclusions:

  • The review addresses unmet needs and challenges in BET inhibition for cancer.
  • Provides insights into current developments and future prospects of BET inhibitors.

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