Open Access
HDACi--going through the mechanisms
Malgorzata Wanczyk1,Katarzyna Roszczenko1,Katarzyna Marcinkiewicz1,Kamil Bojarczuk1,Michal Kowara1,Magdalena Winiarska1
Department of Immunology, Centre of Biostructure Research, Medical University of Warsaw, Banacha 1A, F building, 02-097 Warsaw, Poland
DOI: 10.2741/3691 Volume 16 Issue 1, pp.340-359
Published: 01 January 2011
(This article belongs to the Special Issue Frontiers in molecular medicine)

Histone deacetylases inhibitors (HDACi) have recently emerged as potent antitumor treatment modality. They are currently tested in many phase I, II and III clinical trials as single agents as wells as in combination schemes. They have demonstrated promising antitumor activity and favorable clinical outcome. Histone deacetylases (HDACs) are involved in the process of epigenetic regulation of gene expression. Epigenetic changes are believed to be crucial for the onset and progression of cancer and have recently gained remarkable attention. Since epigenetic regulation of gene expression is a reversible process, targeting histone deacetylases provides a good rationale for anticancer therapy. The acetylation status of histones regulates the organization of chromatin and the access of transcription factors. Moreover, functions of many non-histone proteins are controlled by acetylation. The broad and complicated influences of HDACi on various molecular processes may account for the observed pleiotropic effects. In this review we summarize recent advances in the understanding of biology of HDACs and mechanism of action of their inhibitors.

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Malgorzata Wanczyk, Katarzyna Roszczenko, Katarzyna Marcinkiewicz, Kamil Bojarczuk, Michal Kowara, Magdalena Winiarska. HDACi--going through the mechanisms. Frontiers in Bioscience-Landmark. 2011. 16(1); 340-359.