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Mini-Reviews in Medicinal Chemistry


ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

Histone Deacetylase Inhibitors in the Treatment of Hematological Malignancies

Author(s): A. Petrella, B. Fontanella, A. Carratu, V. Bizzarro, M. Rodriquez and L. Parente

Volume 11 , Issue 6 , 2011

Page: [519 - 527] Pages: 9

DOI: 10.2174/138955711795843347

Price: $65


Histone deacetylases (HDACs) play a central role in the epigenetic regulation of gene expression. Aberrant activity of HDACs has been found in several human cancers leading to the development of HDAC inhibitors (HDACi) as anti-tumors drugs. In fact, over the last years, a number of HDACi have been evaluated in clinical trials; these drugs have the common ability to hyperacetylate both histone and non-histone targets, resulting in a variety of effects on both cancer cells and immune responses. Clinical trials of HDACi conducted in solid tumors and hematological malignancies have shown a better clinical efficacy of these drugs in hematological malignancies. In this review, will be highlighted the mechanisms of action underlying the clinical responses obtained with these drugs and the doubts regarding the use of HDACi in cancer therapy.

Keywords: Histone deacetylases, histone deacetylases inhibitors, hematological malignancies, HDACs, epigenetic, regulation, Aberrant activity, human cancers, inhibitors, HDACi, anti-tumors, hyperacetylate, non-histone

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