HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

Immunol Cell Biol. 2012 Jan;90(1):85-94. doi: 10.1038/icb.2011.100. Epub 2011 Nov 29.


Reversible acetylation mediated by histone deacetylases (HDACs) influences a broad repertoire of physiological processes, many of which are aberrantly controlled in tumor cells. As HDAC inhibition prompts tumor cells to enter apoptosis, small-molecule HDAC inhibitors have been developed as a new class of mechanism-based anti-cancer agent, many of which have entered clinical trials. Although the clinical picture is evolving and the precise utility of HDAC inhibitors remains to be determined, it is noteworthy that certain tumor types undergo a favorable response, in particular hematological malignancies. Vorinostat and romidepsin have been approved for treating cutaneous T-cell lymphoma in patients with progressive, persistent or recurrent disease. Here, we discuss developments in our understanding of molecular events that underlie the anti-cancer effects of HDAC inhibitors and relate this information to the emerging clinical picture for the application of these inhibitors in the treatment of cancer.

Publication types

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

MeSH terms

  • Acetylation / drug effects
  • Antineoplastic Agents / therapeutic use*
  • Depsipeptides / therapeutic use
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Histone Deacetylases / metabolism*
  • Humans
  • Hydroxamic Acids / therapeutic use
  • Lymphoma, T-Cell / drug therapy
  • Lymphoma, T-Cell / enzymology
  • Lymphoma, T-Cell / metabolism
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / metabolism
  • Vorinostat


  • Antineoplastic Agents
  • Depsipeptides
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Vorinostat
  • romidepsin
  • Histone Deacetylases