Physicochemical modifications of histones and their impact on epigenomics

Drug Discov Today. 2014 Sep;19(9):1372-9. doi: 10.1016/j.drudis.2014.05.005. Epub 2014 May 20.

Abstract

The study of histone post-translational modifications (PTMs) has made extraordinary progress over the past few years and many epigenetic modifications have been identified and found to be associated with fundamental biological processes and pathological conditions. Most histone-modifying enzymes produce specific covalent modifications on histone tails that, taken together, elicit complex and concerted processes. An even higher level of complexity is generated by the action of small molecules that are able to modulate pharmacologically epigenetic enzymes and interfere with these biochemical mechanisms. In this article, we provide an overview of histone PTMs by reviewing and discussing them in terms of their physicochemical properties, emphasizing these concepts in view of recent research efforts to elucidate epigenetic mechanisms and devise future epigenetic drugs.

Publication types

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

MeSH terms

  • Drug Design
  • Epigenesis, Genetic*
  • Epigenomics
  • Histones / genetics
  • Histones / metabolism*
  • Humans
  • Protein Processing, Post-Translational*

Substances

  • Histones