Fatty acids as histone deacetylase inhibitors: Old biochemistry tales in a new life sciences town

Drug Discov Today. 2023 May;28(5):103569. doi: 10.1016/j.drudis.2023.103569. Epub 2023 Mar 27.

Abstract

Histone acetylation is a key epigenetic event. Although the keywords fatty acids, histones, and histone acetylation have a long history in biochemistry, these topics continue to attract much attention among researchers. The acetylation of histones is controlled by the activities of histone acetyltransferases (HATs) and histone deacetylases (HDACs). An imbalance in the activities of HATs and HDACs is common in a range of human cancers. Histone deacetylase inhibitors (HDACi) can restore dysregulated histone acetylation profiles in cancer cells and have been identified as promising anti-cancer therapeutics. Short-chain fatty acids mediate anti-cancer effects by inhibiting the activity of HDACs. Recent studies have identified odd-chain fatty acids as novel HDACi. This review summarizes recent findings regarding fatty acids as HDACi in cancer therapy.

Keywords: cancer, epigenetics; fatty acids; histone deacetylase; histone deacetylase inhibitors.

Publication types

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

MeSH terms

  • Biological Science Disciplines*
  • Fatty Acids
  • Histone Acetyltransferases / metabolism
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylases / metabolism
  • Histones
  • Humans
  • Neoplasms* / drug therapy

Substances

  • Histone Deacetylase Inhibitors
  • Histones
  • Fatty Acids
  • Histone Deacetylases
  • Histone Acetyltransferases