The Search for Potent, Small-Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat

Med Res Rev. 2017 Nov;37(6):1373-1428. doi: 10.1002/med.21437. Epub 2017 Feb 9.

Abstract

Histone deacetylases (HDACs) play a crucial role in the remodeling of chromatin, and are involved in the epigenetic regulation of gene expression. In the last decade, inhibition of HDACs came out as a target for specific epigenetic changes associated with cancer and other diseases. Until now, more than 20 HDAC inhibitors (HDACIs) have entered clinical studies, and some of them (e.g., vorinostat, romidepsin) have been approved for the treatment of cutaneous T-cell lymphoma. This review provides an overview of current knowledge, progress, and molecular mechanisms of HDACIs, covering a period from 2011 until 2015.

Keywords: benzamides; cyclic peptides; epigenetics; histone deacetylase inhibitors; hydroxamic acids.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Histone Deacetylase Inhibitors / pharmacology*
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Humans
  • Hydroxamic Acids / therapeutic use
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Small Molecule Libraries / pharmacology*
  • Small Molecule Libraries / therapeutic use*
  • Vorinostat

Substances

  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Small Molecule Libraries
  • Vorinostat