Small molecule inhibitors of histone acetyltransferases and deacetylases are potential drugs for inflammatory diseases

Drug Discov Today. 2014 May;19(5):654-60. doi: 10.1016/j.drudis.2013.11.012. Epub 2013 Nov 21.


Lysine acetylation is a reversible post-translational modification (PTM) of cellular proteins and represents an important regulatory switch in signal transduction. Lysine acetylation, in combination with other PTMs, directs the outcomes as well as the activation levels of important signal transduction pathways such as the nuclear factor (NF)-κB pathway. Small molecule modulators of the 'writers' (HATs) and 'erasers' (HDACs) can regulate the NF-κB pathway in a specific manner. This review focuses on the effects of frequently used HAT and HDAC inhibitors on the NF-κB signal transduction pathway and inflammatory responses, and their potential as novel therapeutics.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Histone Acetyltransferases / antagonists & inhibitors*
  • Histone Acetyltransferases / genetics
  • Histone Acetyltransferases / metabolism
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Histone Deacetylases* / genetics
  • Histone Deacetylases* / metabolism
  • Humans
  • Inflammation / drug therapy
  • Inflammation / enzymology
  • Inflammation / genetics
  • Molecular Sequence Data


  • Anti-Inflammatory Agents
  • Histone Deacetylase Inhibitors
  • Histone Acetyltransferases
  • Histone Deacetylases