HDAC modulation and cell death in the clinic

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• 作者：Carmela Dell'Aversana^a ; Ilaria Lepore^b ; Lucia Altucci^a ; ^b ; ^{lucia.altucci@unina2.it}
• 关键词：Histone deacetylases ; Histone deacetylase inhibitors ; Cancer ; Clinical trials
• 刊名：Experimental Cell Research
• 出版年：2012
• 期刊代码：292_00144827
• 类别：med
• 出版时间：1 July, 2012
• 卷：318
• 期：11
• 页码：1229-1244
• 文件大小：490 K

摘要

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.