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Received for publication April 26, 2005.
Revised June 7, 2005.
Accepted for publication June 8, 2005.
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 non-clinically and in the clinic, in part due to their potential roles in reversing the silenced genes in transformed tumor cells by modulating transcriptional processes. This review is an effort to summarize the non-clinical and clinical status of HDAC inhibitors currently under development in anticancer therapy.
Key words:
Transcriptional coactivators, DNA binding sites, Mechanisms of cell killing/apoptosis, Pharmacokinetics, metabolism and activation, Transcription targets, Tumor suppressors, Angiogenesis
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