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Molecular Pharmacology Fast Forward
First published on June 14, 2005; DOI: 10.1124/mol.105.014167

0026-895X/05/6804-917-932$20.00
Mol Pharmacol 68:917-932, 2005

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MINIREVIEW

Rational Development of Histone Deacetylase Inhibitors as Anticancer Agents: A Review

Milin R. Acharya, Alex Sparreboom, Jürgen Venitz, and William D. Figg

Clinical Pharmacology Research Core, National Cancer Institute, National Institutes of Health, Bethesda, Maryland (M.R.A., A.S., W.D.F.); and Department of Pharmaceutics, School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia (M.R.A., J.V.)

The epigenome is defined by DNA methylation patterns and the associated post-translational modifications of histones. This histone code determines the expression status of individual genes dependent upon their localization on the chromatin. The histone deacetylases (HDACs) play a major role in keeping the balance between the acetylated and deacetylated states of chromatin and eventually regulate gene expression. Recent developments in understanding the cancer cell cycle, specifically the interplay with chromatin control, are providing opportunities for developing mechanism-based therapeutic drugs. Inhibitors of HDACs are under considerable exploration, in part because of their potential roles in reversing the silenced genes in transformed tumor cells by modulating transcriptional processes. This review is an effort to summarize the nonclinical and clinical status of HDAC inhibitors currently under development in anticancer therapy.

Received April 25, 2005; accepted June 8, 2005

Address correspondence to: Dr. William D. Figg, Clinical Pharmacology Research Core, National Cancer Institute, 9000 Rockville Pike, Building 10/Room 5A01, MSC1910, Bethesda, MD 20892. E-mail: wdfigg{at}helix.nih.gov




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