Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight
Thirty Years of HDAC Inhibitors: 2020 Insight and Hindsight
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DOI：
10.1021/acs.jmedchem.0c00830
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发表时间：
2020-11-12
影响因子：
7.3
通讯作者：
Ganesan, A.
中科院分区：
文献类型：
--
作者：
Ho, Terence C. S.;Chan, Alex H. Y.;Ganesan, A.
自从首次报道有效的锌依赖性组蛋白去乙酰化酶（HDAC）抑制剂以来，已经过去了30年。从那时起，五种HDAC抑制剂已获得癌症化疗的监管批准，而其他许多抑制剂正在肿瘤学和其他治疗适应症的临床开发中。本文综述了近30年来生物化学和药物化学方面的进展，重点介绍了区分11种HDAC亚型的选择性抑制剂的设计。
It is now 30 years since the first report of a potent zinc-dependent histone deacetylase (HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory approval for cancer chemotherapy while many others are in clinical development for oncology as well as other therapeutic indications. This Perspective reviews the biological and medicinal chemistry advances over the past 3 decades with an emphasis on the design of selective inhibitors that discriminate between the 11 human HDAC isoforms.