Advances and challenges in understanding histone demethylase biology

Curr Opin Chem Biol. 2016 Aug:33:151-9. doi: 10.1016/j.cbpa.2016.06.021. Epub 2016 Jun 29.

Abstract

Within the last decade we have witnessed significant progress in the field of chromatin methylation, ranging from the discovery that chromatin methylation is reversible, to the identification of two classes of oxidative chromatin demethylases. Multiple genetic and cellular studies emphasize the role of members of the amine oxidase and 2-oxoglutarate oxygenase enzyme families involved in methyl-lysine in physiology and disease. Advances in understanding of the underlying biochemistry have resulted in development of first series of clinical inhibitors and tool compounds which continue to resolve and help understand the complex relationships between chromatin modification, control of gene expression and metabolic states.

Publication types

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

MeSH terms

  • Catalysis
  • Clinical Trials as Topic
  • Enzyme Inhibitors / pharmacology
  • Enzyme Inhibitors / therapeutic use
  • Epigenesis, Genetic
  • Genomics
  • Histone Demethylases / antagonists & inhibitors
  • Histone Demethylases / metabolism*
  • Histones / chemistry
  • Histones / metabolism
  • Humans
  • Lysine / metabolism
  • Methylation

Substances

  • Enzyme Inhibitors
  • Histones
  • Histone Demethylases
  • Lysine