IMR Press / FBL / Volume 16 / Issue 1 / DOI: 10.2741/3691

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.

Open Access Article
HDACi--going through the mechanisms
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1 Department of Immunology, Centre of Biostructure Research, Medical University of Warsaw, Banacha 1A, F building, 02-097 Warsaw, Poland
2 Department of Pharmacology Weill Cornell Medical College and Graduate School of Medical Sciences of Cornell University, New York, USA
Academic Editor:Anna Czarnecka
Front. Biosci. (Landmark Ed) 2011, 16(1), 340–359;
Published: 1 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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