Improving understanding of chromatin regulatory proteins and potential implications for drug discovery

Expert Rev Proteomics. 2016;13(4):435-45. doi: 10.1586/14789450.2016.1159960. Epub 2016 Mar 17.

Abstract

Many epigenetic-based therapeutics, including drugs such as histone deacetylase inhibitors, are now used in the clinic or are undergoing advanced clinical trials. The study of chromatin-modifying proteins has benefited from the rapid advances in high-throughput sequencing methods, the organized efforts of major consortiums and by individual groups to profile human epigenomes in diverse tissues and cell types. However, while such initiatives have carefully characterized healthy human tissue, disease epigenomes and drug-epigenome interactions remain very poorly understood. Reviewed here is how high-throughput sequencing improves our understanding of chromatin regulator proteins and the potential implications for the study of human disease and drug development and discovery.

Keywords: Epigenetics; HDAC inhibitors; chromatin modifications; high-throughput sequencing; histone acetylation.

Publication types

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

MeSH terms

  • Animals
  • Chromatin Assembly and Disassembly*
  • Drug Discovery / methods*
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histone Deacetylases / metabolism*
  • Histones / metabolism*
  • Humans
  • Protein Methyltransferases / antagonists & inhibitors
  • Protein Methyltransferases / metabolism*
  • Protein Processing, Post-Translational*

Substances

  • Histone Deacetylase Inhibitors
  • Histones
  • Protein Methyltransferases
  • Histone Deacetylases