Rational Development of Histone Deacetylase Inhibitors as Anticancer Agents: A Review
- 1 October 2005
- journal article
- review article
- Published by Elsevier in Molecular Pharmacology
- Vol. 68 (4) , 917-932
- https://doi.org/10.1124/mol.105.014167
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.Keywords
This publication has 172 references indexed in Scilit:
- CLINICAL DEVELOPMENT OF HISTONE DEACETYLASE INHIBITORS AS ANTICANCER AGENTSAnnual Review of Pharmacology and Toxicology, 2005
- Identification of genes up-regulated by histone deacetylase inhibition with cDNA microarray and exploration of epigenetic alterations on hepatoma cellsJournal of Hepatology, 2004
- Apicidin is a histone deacetylase inhibitor with anti-invasive and anti-angiogenic potentialsBiochemical and Biophysical Research Communications, 2004
- Selective Growth Inhibition of Tumor Cells by a Novel Histone Deacetylase Inhibitor, NVP-LAQ824Cancer Research, 2004
- Inhibition of hypoxia-induced angiogenesis by FK228, a specific histone deacetylase inhibitor, via suppression of HIF-1α activityBiochemical and Biophysical Research Communications, 2002
- Trichostatin A, an inhibitor of histone deacetylase, inhibits hypoxia-induced angiogenesisExpert Opinion on Investigational Drugs, 2001
- Phylogenetic Classification of Prokaryotic and Eukaryotic Sir2-like ProteinsBiochemical and Biophysical Research Communications, 2000
- The Hallmarks of CancerCell, 2000
- Butyric acid and pivaloyloxymethyl butyrate, AN-9, a novel butyric acid derivative, induce apoptosis in HL-60 cellsZeitschrift für Krebsforschung und Klinische Onkologie, 1997
- Disposition of Phenylbutyrate and its Metabolites, Phenylacetate and PhenylacetylglutamineThe Journal of Clinical Pharmacology, 1995