Abstract
Epigenetics as well as post-translational modifications of proteins are emerging as novel attractive targets for anti-cancer therapy. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are two classes of enzymes regulating histone acetylation and whose altered activity has been identified in several cancers. In particular, imbalance in histone acetylation can lead to changes in chromatin structure and transcriptional dysregulation of genes that are involved in the control of proliferation, cell-cycle progression, differentiation and/or apoptosis. In addition, several non histone protein substrates such as transcription factors, chaperone proteins or tubulin, undergo acetylation as key post-translation modification regulating their half-life and function. On this regard, several inhibitors of HDAC, selected by academic as well as industrial research, have been recently shown to induce growth arrest and apoptosis in a variety of human cancer cells and have been patented as anti-cancer agents. Although several clinical studies with HDAC inhibitors are ongoing, their mechanism of action cannot be solely attributed to the level of histone acetylation and molecular basis for their tumor selectivity remains unknown, presenting a challenge for the cancer research community.
Keywords: Histone deacetylase, histone deacetylase inhibitors, combination therapy, cancer
Recent Patents on Anti-Cancer Drug Discovery
Title: Histone Deacetylase Inhibitors: A New Wave of Molecular Targeted Anticancer Agents
Volume: 2 Issue: 2
Author(s): Alfredo Budillon, Elena Di Gennaro, Francesca Bruzzese, Monia Rocco, Giuseppe Manzo and Michele Caraglia
Affiliation:
Keywords: Histone deacetylase, histone deacetylase inhibitors, combination therapy, cancer
Abstract: Epigenetics as well as post-translational modifications of proteins are emerging as novel attractive targets for anti-cancer therapy. Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are two classes of enzymes regulating histone acetylation and whose altered activity has been identified in several cancers. In particular, imbalance in histone acetylation can lead to changes in chromatin structure and transcriptional dysregulation of genes that are involved in the control of proliferation, cell-cycle progression, differentiation and/or apoptosis. In addition, several non histone protein substrates such as transcription factors, chaperone proteins or tubulin, undergo acetylation as key post-translation modification regulating their half-life and function. On this regard, several inhibitors of HDAC, selected by academic as well as industrial research, have been recently shown to induce growth arrest and apoptosis in a variety of human cancer cells and have been patented as anti-cancer agents. Although several clinical studies with HDAC inhibitors are ongoing, their mechanism of action cannot be solely attributed to the level of histone acetylation and molecular basis for their tumor selectivity remains unknown, presenting a challenge for the cancer research community.
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Alfredo Budillon , Elena Di Gennaro , Francesca Bruzzese , Monia Rocco , Giuseppe Manzo and Michele Caraglia , Histone Deacetylase Inhibitors: A New Wave of Molecular Targeted Anticancer Agents, Recent Patents on Anti-Cancer Drug Discovery 2007; 2 (2) . https://dx.doi.org/10.2174/157489207780832450
DOI https://dx.doi.org/10.2174/157489207780832450 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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