Design of small molecule epigenetic modulators

Bioorg Med Chem Lett. 2014 Jan 1;24(1):21-32. doi: 10.1016/j.bmcl.2013.11.001. Epub 2013 Nov 13.

Abstract

The field of epigenetics has expanded rapidly to reveal multiple new targets for drug discovery. The functional elements of the epigenomic machinery can be categorized as writers, erasers and readers, and together these elements control cellular gene expression and homeostasis. It is increasingly clear that aberrations in the epigenome can underly a variety of diseases, and thus discovery of small molecules that modulate the epigenome in a specific manner is a viable approach to the discovery of new therapeutic agents. In this Digest, the components of epigenetic control of gene expression will be briefly summarized, and efforts to identify small molecules that modulate epigenetic processes will be described.

Keywords: Acetyllysine; Epigenetic; Histone; Methylarginine; Methyllysine.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Drug Design*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Epigenesis, Genetic / drug effects*
  • Epigenomics*
  • Histone Demethylases / antagonists & inhibitors
  • Histone Demethylases / genetics*
  • Histone Demethylases / metabolism
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Transferases / antagonists & inhibitors
  • Transferases / genetics*
  • Transferases / metabolism

Substances

  • Enzyme Inhibitors
  • Histone Demethylases
  • Transferases