Rational development of histone deacetylase inhibitors as anticancer agents: A review

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

*Corresponding author for this work

Research output: Contribution to journalShort surveypeer-review

218 Scopus citations


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.

Original languageEnglish
Pages (from-to)917-932
Number of pages16
JournalMolecular Pharmacology
Issue number4
StatePublished - Oct 2005
Externally publishedYes


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