摘要
组蛋白去乙酰化酶(HDACs)在癌症的增殖和传播中起重要作用,并且是有希望的表观遗传药物靶标。具有锌结合异羟肟酸盐片段的HDAC抑制剂伏立诺他已经被临床批准。然而,含有异羟肟酸的HDAC抑制剂经常受到获得性或内在性药物抗性的阻碍,并可能导致肿瘤侵袭性增强。为了克服异羟肟酸HDAC抑制剂的这些缺点,最近开发了一系列这种化合物类的多模态衍生物,包括具有不同的锌结合基团的多模态衍生物,并显示出有希望的抗癌活性。这篇综述提供了这些概念上新的HDAC抑制剂的化学和多效抗癌模式的概述。
关键词: 抗癌药物,表观遗传学,组蛋白脱乙酰酶,激酶,DNA靶向,HDAC抑制剂,杂合分子
图形摘要
Current Cancer Drug Targets
Title:Multimodal HDAC Inhibitors with Improved Anticancer Activity
Volume: 18 Issue: 1
关键词: 抗癌药物,表观遗传学,组蛋白脱乙酰酶,激酶,DNA靶向,HDAC抑制剂,杂合分子
摘要: Histone deacetylases (HDACs) play a significant role in the proliferation and dissemination of cancer and represent promising epigenetic drug targets. The HDAC inhibitor vorinostat featuring a zinc-binding hydroxamate fragment was already clinically approved. However, HDAC inhibitors containing hydroxamic acids are often hampered by acquired or intrinsic drug resistance and may lead to enhanced tumor aggressiveness. In order to overcome these drawbacks of hydroxamate HDAC inhibitors, a series of multimodal derivatives of this compound class, including such with different zinc-binding groups, was recently developed and showed promising anticancer activity. This review provides an overview of the chemistry and pleiotropic anticancer modes of action of these conceptually new HDAC inhibitors.
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Cite this article as:
Multimodal HDAC Inhibitors with Improved Anticancer Activity, Current Cancer Drug Targets 2018; 18 (1) . https://dx.doi.org/10.2174/1568009617666170206102613
DOI https://dx.doi.org/10.2174/1568009617666170206102613 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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