Toxoplasma histone acetylation remodelers as novel drug targets

Expert Rev Anti Infect Ther. 2012 Oct;10(10):1189-201. doi: 10.1586/eri.12.100.

Abstract

Toxoplasma gondii is a leading cause of neurological birth defects and a serious opportunistic pathogen. The authors and others have found that Toxoplasma uses a unique nucleosome composition supporting a fine gene regulation together with other factors. Post-translational modifications in histones facilitate the establishment of a global chromatin environment and orchestrate DNA-related biological processes. Histone acetylation is one of the most prominent post-translational modifications influencing gene expression. Histone acetyltransferases and histone deacetylases have been intensively studied as potential drug targets. In particular, histone deacetylase inhibitors have activity against apicomplexan parasites, underscoring their potential as a new class of antiparasitic compounds. In this review, we summarize what is known about Toxoplasma histone acetyltransferases and histone deacetylases, and discuss the inhibitors studied to date. Finally, the authors discuss the distinct possibility that the unique nucleosome composition of Toxoplasma, which harbors a nonconserved H2Bv variant histone, might be targeted in novel therapeutics directed against this parasite.

Publication types

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

MeSH terms

  • Acetylation
  • Amino Acid Sequence
  • Antiparasitic Agents / therapeutic use
  • Chromatin / metabolism
  • Histone Acetyltransferases / genetics
  • Histone Acetyltransferases / metabolism
  • Histone Deacetylase Inhibitors / therapeutic use
  • Histone Deacetylases / genetics
  • Histone Deacetylases / metabolism
  • Histones / chemistry
  • Histones / metabolism*
  • Humans
  • Molecular Sequence Data
  • Nucleosomes / metabolism
  • Protein Processing, Post-Translational
  • Sequence Alignment
  • Toxoplasma / genetics*
  • Toxoplasmosis / drug therapy*
  • Toxoplasmosis / genetics

Substances

  • Antiparasitic Agents
  • Chromatin
  • Histone Deacetylase Inhibitors
  • Histones
  • Nucleosomes
  • Histone Acetyltransferases
  • Histone Deacetylases