靶向DNA和组蛋白去乙酰化酶的双重抑制剂

Chen Chen, Xinying Yang, Xuben Hou, H. Fang
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引用次数: 0

摘要

组蛋白去乙酰化酶(hdac)调节组蛋白的乙酰化状态和染色质的结构状态。抑制HDAC后,染色质结构变得松弛,导致DNA暴露于DNA干扰剂中,最终导致DNA功能障碍。近年来,越来越多的针对DNA和hdac的双重抑制剂被报道用于癌症治疗。本文综述了DNA和hdac双重抑制剂的研究现状,总结了它们的药理特性,并对它们在该领域的发展趋势进行了展望。
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Dual Inhibitors Targeting DNA and Histone Deacetylases
Abstract Histone deacetylases (HDACs) regulate the acetylation status of histones and structural status of chromatin. The chromatin structure becomes relaxed after inhibition of HDAC, leading to DNA exposed to DNA disrupting agents, and eventually causing DNA dysfunction. Recently, more and more dual inhibitors targeting DNA and HDACs have been reported to be applied to cancer treatment. In this review, we describe the current status of dual inhibitors targeting DNA and HDACs, summarize their pharmacological characters, and predict their further trend in the field.
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审稿时长
15 weeks
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