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组蛋白去乙酰化酶的抑制作用。

Inhibition of histone deacetylases.

作者信息

Liu Cheng, Xu Dawei

机构信息

Department of Medicine, Division of Hematology, Karolinska Hospital, Stockholm, Sweden.

出版信息

Methods Mol Biol. 2004;287:87-97. doi: 10.1385/1-59259-828-5:087.

DOI:10.1385/1-59259-828-5:087
PMID:15273406
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3623540/
Abstract

Reversible histone acetylation, governed dynamically by histone acetyltransferases (HATs) and histone deacetylases (HDACs), plays a pivotal role in regulation of gene expression through remodeling chromatin structure. Manipulation of the equilibrium between acetylation and deacetylation of histones by specific HDAC inhibitors is thus a useful tool to study functional role(s) for histone hyper-/hypoacetylation in controlling gene transcription and many other cellular activities. By using the trans-activating effect of trichostatin A (TSA), a widely used HDAC inhibitor, on the telomerase reverse transcriptase (hTERT) gene as an example, we summarize various aspects of HDAC inhibitors and provide a general strategy for their in vitro application in studies of gene regulation.

摘要

可逆性组蛋白乙酰化由组蛋白乙酰转移酶（HATs）和组蛋白去乙酰化酶（HDACs）动态调控，通过重塑染色质结构在基因表达调控中起关键作用。因此，用特定的HDAC抑制剂操纵组蛋白乙酰化与去乙酰化之间的平衡，是研究组蛋白高乙酰化/低乙酰化在控制基因转录及许多其他细胞活动中的功能作用的有用工具。以广泛使用的HDAC抑制剂曲古抑菌素A（TSA）对端粒酶逆转录酶（hTERT）基因的反式激活作用为例，我们总结了HDAC抑制剂的各个方面，并提供了其在基因调控研究中体外应用的一般策略。

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