Table of Contents
ISRN Cell Biology
Volume 2012, Article ID 130360, 12 pages
Review Article

Overview of the Classical Histone Deacetylase Enzymes and Histone Deacetylase Inhibitors

1Epigenomic Medicine, Baker IDI Heart & Diabetes Institute, Alfred Medical Research and Education Precinct, Melbourne, VIC 8008, Australia
2Department of Pathology, The University of Melbourne, Parkville, VIC 3010, Australia

Received 25 September 2011; Accepted 12 October 2011

Academic Editors: A. Hergovich and R. S. Samant

Copyright © 2012 Katherine Ververis and Tom C. Karagiannis. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


The important role of histone deacetylase enzymes in regulating gene expression, cellular proliferation, and survival has made them attractive targets for the development of histone deacetylase inhibitors as anticancer drugs. Suberoylanilide hydroxamic acid (Vorinostat, Zolinza), a structural analogue of the prototypical Trichostatin A, was approved by the US Food and Drug Administration for the treatment of advanced cutaneous T-cell lymphoma in 2006. This was followed by approval of the cyclic peptide, depsipeptide (Romidepsin, Istodax) for the same disease in 2009. Currently numerous histone deacetylase inhibitors are undergoing preclinical and clinical trials for the treatment of hematological and solid malignancies. Most of these studies are focused on combinations of histone deacetylase inhibitors with other therapeutic modalities, particularly conventional chemotherapeutics and radiotherapy. The aim of this paper is to provide an overview of the classical histone deacetylase enzymes and histone deacetylase inhibitors with an emphasis on potential combination therapies.