Histone Deacetylases (HDACs): Evolution, Specificity, Role in Transcriptional Complexes, and Pharmacological Actionability

Genes (Basel). 2020 May 15;11(5):556. doi: 10.3390/genes11050556.

Abstract

Histone deacetylases (HDACs) are evolutionary conserved enzymes which operate by removing acetyl groups from histones and other protein regulatory factors, with functional consequences on chromatin remodeling and gene expression profiles. We provide here a review on the recent knowledge accrued on the zinc-dependent HDAC protein family across different species, tissues, and human pathologies, specifically focusing on the role of HDAC inhibitors as anti-cancer agents. We will investigate the chemical specificity of different HDACs and discuss their role in the human interactome as members of chromatin-binding and regulatory complexes.

Keywords: HDAC; HDAC inhibitors; HDACi; cancer; chromatin; epigenetics; epigenomics; gene networks; histone deacetylases; phylogenesis.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Histone Deacetylases / genetics*
  • Histones / genetics
  • Humans
  • Neoplasms / genetics*
  • Neoplasms / therapy
  • Substrate Specificity / genetics
  • Transcription Factors / genetics*

Substances

  • Antineoplastic Agents
  • Histone Deacetylase Inhibitors
  • Histones
  • Transcription Factors
  • Histone Deacetylases