Journal
EXPERIMENTAL CELL RESEARCH
Volume 318, Issue 11, Pages 1229-1244Publisher
ELSEVIER INC
DOI: 10.1016/j.yexcr.2012.01.025
Keywords
Histone deacetylases; Histone deacetylase inhibitors; Cancer; Clinical trials
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Funding
- EU (APO-SYS) [200767]
- Associazione Italiana per la Ricerca sul cancro (AIRC)
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Histone acetyltransferases (HATs) and histone deacetylases (HDACs) are two opposing classes of enzymes, which finely regulate the balance of histone acetylation affecting chromatin packaging and gene expression. Imbalanced acetylation has been associated with carcinogenesis and cancer progression. In contrast to genetic mutations, epigenetic changes are potentially reversible. This implies that epigenetic alterations are amenable to pharmacological interventions. Accordingly, some epigenetic-based drugs (epidrugs) have been approved by the Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for cancer treatment. Here, we focus on the biological features of HDAC inhibitors (HDACis), analyzing the mechanism(s) of action and their current use in clinical practice. (C) 2012 Elsevier Inc. All rights reserved.
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