Isoform-selective histone deacetylase inhibitors

Chem Soc Rev. 2008 Jul;37(7):1402-13. doi: 10.1039/b703830p. Epub 2008 May 8.


Histone deacetylase (HDAC) proteins are transcription regulators linked to cancer. As a result, multiple small molecule HDAC inhibitors are in various phases of clinical trials as anti-cancer drugs. The majority of HDAC inhibitors non-selectively influence the activities of eleven human HDAC isoforms, which are divided into distinct classes. This tutorial review focuses on the recent progress toward the identification of class-selective and isoform-selective HDAC inhibitors. The emerging trends suggest that subtle differences in the active sites of the HDAC isoforms can be exploited to dictate selectivity.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Binding Sites
  • Cell Proliferation / drug effects*
  • Drug Design
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Histone Deacetylase Inhibitors*
  • Histone Deacetylases / chemistry
  • Humans
  • Hydroxamic Acids / pharmacology
  • Protein Isoforms / antagonists & inhibitors*
  • Protein Isoforms / chemistry
  • Tumor Cells, Cultured
  • Vorinostat


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Protein Isoforms
  • trichostatin A
  • Vorinostat
  • Histone Deacetylases