Histone deacetylase (HDACs) inhibitors: Clinical applications

Prog Mol Biol Transl Sci. 2023:198:119-152. doi: 10.1016/bs.pmbts.2023.02.011. Epub 2023 Mar 31.

Abstract

Histone Deacetylases (HDACs) deacetylate lysine residues in histone and non-histone proteins. HDACs have been implicated in several diseases, including cancer, neurodegeneration, and cardiovascular disease. HDACs play an essential role in gene transcription, cell survival, growth, and proliferation, with histone hypoacetylation as one of the critical downstream signatures. HDAC inhibitors (HDACi) regulate gene expression epigenetically by restoring acetylation levels. Contrarily, only few HDACi have received FDA approval, and the majority are presently undergoing clinical trials to ascertain their effectiveness in the prevention and treatment of disease. In this book chapter, we give a detailed list of HDAC classes, and their functions in advancing diseases like cancer, cardiovascular, and neurodegeneration. Furthermore we touch upon novel and promising HDACi therapy approaches in the relevance of the current clinical scenario.

Keywords: Cancer; Cardiovascular; HDACi; HDACs; Neurodegeneration.

MeSH terms

  • Acetylation
  • Cardiovascular Diseases* / drug therapy
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use
  • Histone Deacetylases*
  • Histones
  • Humans

Substances

  • Histone Deacetylases
  • Histones
  • Histone Deacetylase Inhibitors