Chromatin Proteins and Modifications as Drug Targets

Nature. 2013 Oct 24;502(7472):480-8. doi: 10.1038/nature12751.


A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.

Publication types

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

MeSH terms

  • Animals
  • Chromatin / chemistry
  • Chromatin / drug effects*
  • Chromatin / enzymology
  • Chromatin / metabolism*
  • Histone Demethylases / antagonists & inhibitors
  • Histone Demethylases / metabolism
  • Histone Methyltransferases
  • Histone-Lysine N-Methyltransferase / antagonists & inhibitors
  • Histone-Lysine N-Methyltransferase / metabolism
  • Humans
  • Molecular Targeted Therapy*
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Protein Structure, Tertiary / drug effects


  • Chromatin
  • Histone Demethylases
  • KDM1A protein, human
  • Histone Methyltransferases
  • Histone-Lysine N-Methyltransferase