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

Milin R. Acharya; Alex Sparreboom; Jürgen Venitz; William D. Figg

doi:10.1124/mol.105.014167

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 journal › Short survey › peer-review

220 Scopus citations

Abstract

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 language	English
Pages (from-to)	917-932
Number of pages	16
Journal	Molecular Pharmacology
Volume	68
Issue number	4
DOIs	https://doi.org/10.1124/mol.105.014167
State	Published - Oct 2005
Externally published	Yes

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title = "Rational development of histone deacetylase inhibitors as anticancer agents: A review",

abstract = "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.",

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AU - Figg, William D.

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AB - 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.

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

Abstract

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