Bieliauskas Anton V, Pflum Mary Kay H
Department of Chemistry, Wayne State University, Detroit, MI 48202, USA.
Chem Soc Rev. 2008 Jul;37(7):1402-13. doi: 10.1039/b703830p. Epub 2008 May 8.
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.
组蛋白去乙酰化酶（HDAC）蛋白是与癌症相关的转录调节因子。因此，多种小分子HDAC抑制剂正处于作为抗癌药物的不同临床试验阶段。大多数HDAC抑制剂非选择性地影响11种人类HDAC亚型的活性，这些亚型被分为不同的类别。本教程综述重点关注在鉴定类别选择性和亚型选择性HDAC抑制剂方面的最新进展。新出现的趋势表明，可以利用HDAC亚型活性位点的细微差异来决定选择性。
