The nonepigenetic role for small molecule histone deacetylase inhibitors in the regulation of cardiac function

Future Med Chem. 2019 Jun;11(11):1345-1356. doi: 10.4155/fmc-2018-0311. Epub 2019 Jun 4.

Abstract

Eight million US adults are projected to suffer from heart failure (HF) by 2030. Of concern, 5-year mortality rates following HF diagnosis approximate 40%. Small molecule histone deacetylase (HDAC) inhibitors have demonstrated efficacy for the treatment and reversal of HF. Historically, HDACs were studied as regulators of nucleosomal histones, in which lysine deacetylation on histone tails changed DNA-histone protein electrostatic interactions, leading to chromatin condensation and changes in gene expression. However, recent proteomics studies have demonstrated that approximately 4500 proteins can be acetylated in various tissues; the function of most of these remains unknown. This Review will focus on the nonepigenetic role for lysine acetylation in the heart, with a focus on nonepigenetic actions for HDAC inhibitors on cardiac function.

Keywords: HDACs; heart failure; histone deacetylase; lysine acetylation; mitochondrial acetylation; sarcomere protein acetylation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Acetylation / drug effects
  • Animals
  • Heart / drug effects
  • Heart Failure / drug therapy*
  • Heart Failure / metabolism
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Histone Deacetylases / metabolism
  • Humans
  • Lysine / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Small Molecule Libraries / therapeutic use*

Substances

  • Histone Deacetylase Inhibitors
  • Small Molecule Libraries
  • Histone Deacetylases
  • Lysine