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Roles of Histone Deacetylases and Inhibitors in Anticancer Therapy

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Biotechnology Unit, University of Ribeirão Preto, Ribeirão Preto SP CEP 14096-900, Brazil
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College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, SK S7N 5C9, Canada
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Medicine School, University of Ribeirão Preto, Ribeirão Preto SP CEP 14096-900, Brazil
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Pharmaceutical Sciences School, University of Ribeirão Preto, Ribeirão Preto SP CEP 14096-900, Brazil
*
Authors to whom correspondence should be addressed.
Cancers 2020, 12(6), 1664; https://doi.org/10.3390/cancers12061664
Received: 10 April 2020 / Revised: 19 May 2020 / Accepted: 19 May 2020 / Published: 23 June 2020
Histones are the main structural proteins of eukaryotic chromatin. Histone acetylation/ deacetylation are the epigenetic mechanisms of the regulation of gene expression and are catalyzed by histone acetyltransferases (HAT) and histone deacetylases (HDAC). These epigenetic alterations of DNA structure influence the action of transcription factors which can induce or repress gene transcription. The HATs catalyze acetylation and the events related to gene transcription and are also responsible for transporting newly synthesized histones from the cytoplasm to the nucleus. The activity of HDACs is mainly involved in silencing gene expression and according to their specialized functions are divided into classes I, II, III and IV. The disturbance of the expression and mutations of HDAC genes causes the aberrant transcription of key genes regulating important cancer pathways such as cell proliferation, cell-cycle regulation and apoptosis. In view of their role in cancer pathways, HDACs are considered promising therapeutic targets and the development of HDAC inhibitors is a hot topic in the search for new anticancer drugs. The present review will focus on HDACs I, II and IV, the best known inhibitors and potential alternative inhibitors derived from natural and synthetic products which can be used to influence HDAC activity and the development of new cancer therapies. View Full-Text
Keywords: histone deacetylases; histone deacetylase inhibitors; histones; cancer; curcumin; chalcones; histone acetyltransferase histone deacetylases; histone deacetylase inhibitors; histones; cancer; curcumin; chalcones; histone acetyltransferase
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Verza, F.A.; Das, U.; Fachin, A.L.; Dimmock, J.R.; Marins, M. Roles of Histone Deacetylases and Inhibitors in Anticancer Therapy. Cancers 2020, 12, 1664.

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