HDAC1/3 dual selective inhibitors - new therapeutic agents for the potential treatment of cancer.
HDAC1/3 dual selective inhibitors - new therapeutic agents for the potential treatment of cancer.
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HDAC1/3 双重选择性抑制剂 - 用于潜在治疗癌症的新治疗药物。
DOI：
10.5582/ddt.2014.01034
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发表时间：
2014-10
期刊：
影响因子：
--
通讯作者：
Xu, Wenfang
中科院分区：
文献类型：
--
作者：
Li, Xiaoyang;Xu, Wenfang
组蛋白脱乙酰酶(HDAC)作为抗癌药物靶点已引起人们的极大兴趣，许多HDAC抑制剂(HDACIs)已在治疗特定肿瘤方面显示出临床疗效。然而，所有这些药物都有明显的毒性，包括疲劳、恶心、呕吐、血小板减少和中性粒细胞减少。因此，正在加大努力开发耐受性更好、不良反应更少的选择性HDACI。本文主要介绍了基于N-羟基肉桂酰胺的HDAC1/3双重抑制剂，并概述了这些抑制剂的抗癌潜力。由于选择性Ι1/3抑制剂在临床上可能比选择性PAN-HDACIs和选择性类HDACIs引起的不良反应少，因此有必要进一步研究它们的抗癌作用机制和优化它们的结构。
Histone deacetylases (HDACs) have attracted a great deal of interest as anticancer drug targets, and many HDAC inhibitors (HDACIs) have displayed clinical efficacy in treating specific tumors. However, all of these agents have significant toxicity, including fatigue, nausea, vomiting, thrombocytopenia, and neutropenia. Thus, increased effort is being directed toward developing selective HDACIs that are tolerated better and cause fewer adverse reactions. This article focuses mainly on the N-hydroxycinnamamide-based HDAC 1/3 dual inhibitors, and this article outlines the anticancer potential of these inhibitors. Since selective HDAC1/3 inhibitors may cause fewer adverse reactions than selective pan-HDACIs and selective Class Ι inhibitors in clinical settings, further study of their mechanism of anticancer activity and optimization of their structure is warranted.
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