Epigenetic small molecule modulators of histone and DNA methylation

Curr Opin Chem Biol. 2018 Aug:45:73-85. doi: 10.1016/j.cbpa.2018.03.003. Epub 2018 Mar 24.

Abstract

DNA and histone methylation belong to the key regulatory components in the epigenetic machinery, and dysregulations of these processes have been associated with various human diseases. Small molecule modulators of these epigenetic targets are highly valuable both as chemical probes to study the biological roles of the target proteins, and as potential therapeutics. Indeed, recent years have seen the discovery of chemical modulators of several epigenetic targets, some of which are already marketed drugs or undergoing clinical trials. In this review, we will focus on small molecule modulators of DNA and histone methylation.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • DNA Methylation / drug effects*
  • DNA Modification Methylases / antagonists & inhibitors
  • DNA Modification Methylases / metabolism
  • Drug Discovery* / methods
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Epigenesis, Genetic / drug effects*
  • Histone Demethylases / antagonists & inhibitors
  • Histone Demethylases / metabolism
  • Histone-Lysine N-Methyltransferase / antagonists & inhibitors
  • Histone-Lysine N-Methyltransferase / metabolism
  • Histones / genetics*
  • Histones / metabolism
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Protein-Arginine N-Methyltransferases / antagonists & inhibitors
  • Protein-Arginine N-Methyltransferases / metabolism
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histones
  • Small Molecule Libraries
  • Histone Demethylases
  • DNA Modification Methylases
  • Protein-Arginine N-Methyltransferases
  • Histone-Lysine N-Methyltransferase