Natural Product Inhibitors of Histone Deacetylases as New Anticancer Agents

Curr Protein Pept Sci. 2018;19(3):333-340. doi: 10.2174/1389203718666170106101133.

Abstract

Acetylation and deactylation of histones are important determinants of gene expression. Histone deacetylases (HDACs) remove acetyl groups from histones leading to suppression and regulation of epigenetic gene expression. Current studies have demonstrated that HDAC-inhibitors (HDACIs) inducing histone hyperacetylation are promising novel agents in cancer treatment. HDACIs have been shown to have significant anticancer effects with negligible toxicity in the preclinical studies. Ongoing clinial trials are being performed to investigate the efficiency of HDACIs in human cancers. We have reviewed the current knowledge about the molecular mechanisms of action of HDACIs and the outcome of clinical studies using HDACIs in the therapy of several cancers.

Keywords: Histone acetylation; anticancer agents; epigenetic; hematologic malignancies; histone deacetylase inhibitors; solid tumors.

Publication types

  • Review

MeSH terms

  • Acetylation / drug effects
  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Biological Products / pharmacology
  • Biological Products / therapeutic use*
  • Epigenesis, Genetic / drug effects
  • Gene Expression Regulation, Neoplastic / drug effects
  • Histone Deacetylase Inhibitors / chemistry
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Histone Deacetylases / metabolism
  • Histones / genetics
  • Histones / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Neoplasms / metabolism
  • Neoplasms / pathology

Substances

  • Antineoplastic Agents
  • Biological Products
  • Histone Deacetylase Inhibitors
  • Histones
  • Histone Deacetylases