Histone acetyltransferases are crucial regulators in NF-κB mediated inflammation

Drug Discov Today. 2011 Jun;16(11-12):504-11. doi: 10.1016/j.drudis.2011.03.009. Epub 2011 Apr 6.

Abstract

Post-translational modifications of proteins, such as acetylation, are important regulatory events in eukaryotic cells. Reversible acetylations of histones and non-histone proteins regulate gene expression and protein activity. Acetylation levels of proteins are regulated by a dynamic equilibrium between acetylation by (histone) acetyltransferases and deacetylation by (histone) deacetylases. Alterations in this equilibrium can result in pathological states. Inflammation is a physiological response that, under certain conditions, turns into a disease. This review focuses on the crucial regulatory roles of protein acetylation in NF-κB-mediated inflammation and the potential applications of small-molecule inhibitors of acetylation for the treatment of inflammatory diseases.

Publication types

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

MeSH terms

  • Acetylation
  • Animals
  • Histone Acetyltransferases / antagonists & inhibitors*
  • Humans
  • Inflammation / drug therapy
  • Inflammation / enzymology*
  • Inflammation / immunology
  • NF-kappa B / genetics
  • NF-kappa B / immunology
  • NF-kappa B / metabolism*
  • Protein Processing, Post-Translational
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / therapeutic use

Substances

  • NF-kappa B
  • Small Molecule Libraries
  • Histone Acetyltransferases