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组蛋白去乙酰化酶与癌症。

Histone deacetylases and cancer.

机构信息

Cellular Differentiation Group, Cancer Epigenetics and Biology Program, Bellvitge Biomedical Research Institute, Av. Gran Via s/n km 2.7, 08908 L'Hospitalet, Barcelona, Spain.

出版信息

Mol Oncol. 2012 Dec;6(6):579-89. doi: 10.1016/j.molonc.2012.07.003. Epub 2012 Aug 27.

Abstract

Reversible acetylation of histone and non-histone proteins is one of the most abundant post-translational modifications in eukaryotic cells. Protein acetylation and deacetylation are achieved by the antagonistic actions of two families of enzymes, histone acetyltransferases (HATs) and histone deacetylases (HDACs). Aberrant protein acetylation, particularly on histones, has been related to cancer while abnormal expression of HDACs has been found in a broad range of cancer types. Therefore, HDACs have emerged as promising targets in cancer therapeutics, and the development of HDAC inhibitors (HDIs), a rapidly evolving area of clinical research. However, the contributions of specific HDACs to a given cancer type remain incompletely understood. The aim of this review is to summarize the current knowledge concerning the role of HDACs in cancer with special emphasis on what we have learned from the analysis of patient samples.

摘要

组蛋白和非组蛋白蛋白质的可逆乙酰化是真核细胞中最丰富的翻译后修饰之一。蛋白质乙酰化和去乙酰化是通过两组酶的拮抗作用实现的,即组蛋白乙酰转移酶(HATs)和组蛋白去乙酰化酶(HDACs)。异常的蛋白质乙酰化,特别是组蛋白上的乙酰化,与癌症有关,而在广泛的癌症类型中发现了 HDAC 的异常表达。因此,HDAC 已成为癌症治疗的有前途的靶点,HDAC 抑制剂(HDIs)的开发是临床研究的一个迅速发展的领域。然而,特定的 HDAC 对特定癌症类型的贡献仍不完全清楚。本综述的目的是总结目前关于 HDAC 在癌症中的作用的知识,特别强调从对患者样本的分析中所学到的内容。

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