Erythropoiesis provides a BRD's eye view of BET protein function

Drug Discov Today Technol. 2016 Mar;19:23-28. doi: 10.1016/j.ddtec.2016.05.004. Epub 2016 Jul 20.

Abstract

Pharmacologic inhibitors of the bromodomain and extra-terminal motif (BET) protein family are in clinical trials for the treatment of hematologic malignancies, yet the functions of individual BET proteins remain largely uncharacterized. We review the molecular roles of BETs in the context of erythropoiesis. Studies in this lineage have provided valuable insights into their mechanisms of action, and helped define the individual and overlapping functions of BET protein family members BRD2, BRD3, and BRD4. These studies have important ramifications for our understanding of the molecular and physiologic roles of BET proteins, and provide a framework for elucidating some of the beneficial and adverse effects of pharmacologic inhibitors.

Publication types

  • Review

MeSH terms

  • Animals
  • Chromatin / metabolism
  • Erythropoiesis / physiology*
  • Humans
  • Nuclear Proteins / antagonists & inhibitors
  • Nuclear Proteins / chemistry
  • Nuclear Proteins / metabolism*
  • Protein Domains*
  • Transcription Factors / antagonists & inhibitors
  • Transcription Factors / chemistry
  • Transcription Factors / metabolism*

Substances

  • Chromatin
  • Nuclear Proteins
  • Transcription Factors