Cytotoxicity mediated by histone deacetylase inhibitors in cancer cells: mechanisms and potential clinical implications.

Cytotoxicity mediated by histone deacetylase inhibitors in cancer cells: mechanisms and potential clinical implications.
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DOI:
10.1158/1078-0432.ccr-08-2787
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发表时间:
2009-06-15
期刊:
Clinical cancer research : an official journal of the American Association for Cancer Research
影响因子:
--
通讯作者:
Schrump DS
Schrump DS
中科院分区:
其他
文献类型:
--
作者:
Schrump DS

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基因表达的表观遗传调控因子的异常表达有助于癌症的发生和发展。近年来,大量的研究工作集中在组蛋白乙酰转移酶(HATs)和组蛋白去乙酰化酶(hdac)在癌细胞中的作用,以及通过抑制hdac来调节基因表达的药物的鉴定。以下综述重点介绍了最近有关HDAC在癌细胞中的表达、HDAC抑制剂介导抗肿瘤活性的多效性机制以及HDAC抑制作为癌症治疗策略的潜在临床意义。
Aberrant expression of epigenetic regulators of gene expression contributes to initiation and progression of cancer. During recent years, considerable research efforts have focused on the role of histone acetyltransferases (HATs) and histone deacetylases (HDACs) in cancer cells, and the identification of pharmacologic agents that modulate gene expression via inhibition of HDACs. The following review highlights recent studies pertaining to HDAC expression in cancer cells, the plieotropic mechanisms by which HDAC inhibitors (HDACi) mediate antitumor activity, and the potential clinical implications of HDAC inhibition as a strategy for cancer therapy.