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分子途径:老药开辟新途径:DNA 损伤反应和自噬交汇点的非组蛋白乙酰化。

Molecular pathways: old drugs define new pathways: non-histone acetylation at the crossroads of the DNA damage response and autophagy.

机构信息

Department of Experimental Oncology, European Institute of Oncology, Milan, Italy.

出版信息

Clin Cancer Res. 2012 May 1;18(9):2436-42. doi: 10.1158/1078-0432.CCR-11-0767. Epub 2012 Apr 18.

Abstract

Histone deacetylases (HDAC) modulate acetylation and the function of histone and non-histone proteins. HDAC inhibitors have been developed to block the aberrant action of HDACs in cancer, and several are in clinical use (vorinostat, romidepsin, and valproic acid). Detailed understanding of their action is lacking, however, and their clinical activity is limited in most cases. Recently, HDACs have been involved in the control of the DNA damage response (DDR) at several levels and in directly regulating the acetylation of a number of DDR proteins (including CtIP and Exo1). Mechanistically, acetylation leads to the degradation of double-strand break repair enzymes through autophagy, providing a novel, direct link between DDR and autophagy. These observations, obtained in yeast cells, should now be translated to mammalian model systems and cancer cells to reveal whether this acetylation link is maintained in mammals, and if and how it is deregulated in cancer. In addition to HDACs, DDR and autophagy have been addressed pharmacologically, suggesting that the acetylation link, if involved in cancer, can be exploited for the design of new anticancer treatments.

摘要

组蛋白去乙酰化酶 (HDAC) 调节组蛋白和非组蛋白蛋白的乙酰化和功能。已经开发了 HDAC 抑制剂来阻断 HDAC 在癌症中的异常作用,并且有几种正在临床使用(伏立诺他、罗米地辛和丙戊酸)。然而,人们对它们的作用机制了解甚少,并且在大多数情况下,它们的临床活性受到限制。最近,HDAC 已在多个层面参与 DNA 损伤反应 (DDR) 的调控,并直接调节许多 DDR 蛋白的乙酰化(包括 CtIP 和 Exo1)。从机制上讲,通过自噬导致双链断裂修复酶的降解,为 DDR 和自噬之间提供了一个新的直接联系。这些在酵母细胞中获得的观察结果现在应该被转化为哺乳动物模型系统和癌细胞,以揭示这种乙酰化联系是否在哺乳动物中保持,以及在癌症中它是否以及如何被失调。除了 HDAC 之外,DDR 和自噬也已在药理学上得到解决,这表明如果乙酰化联系参与癌症,则可以利用它来设计新的抗癌治疗方法。

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