Isoform-selective histone deacetylase inhibitors

被引：272

作者：

Bieliauskas, Anton V. ^{[1
]}

Pflum, Mary Kay H. ^{[1
]}

机构：

[1] Wayne State Univ, Dept Chem, Detroit, MI 48202 USA

来源：

CHEMICAL SOCIETY REVIEWS | 2008年 / 37卷 / 07期

关键词：

D O I：

10.1039/b703830p

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Histone deacetylase (HDAC) proteins are transcription regulators linked to cancer. As a result, multiple small molecule HDAC inhibitors are in various phases of clinical trials as anti-cancer drugs. The majority of HDAC inhibitors non-selectively influence the activities of eleven human HDAC isoforms, which are divided into distinct classes. This tutorial review focuses on the recent progress toward the identification of class-selective and isoform-selective HDAC inhibitors. The emerging trends suggest that subtle differences in the active sites of the HDAC isoforms can be exploited to dictate selectivity.

引用

页码：1402 / 1413

页数：12

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