HDAC1/3 dual selective inhibitors - New therapeutic agents for the potential treatment of cancer

被引:11
|
作者
Li, Xiaoyang [1 ]
Xu, Wenfang [1 ]
机构
[1] Shandong Univ, Sch Pharm, Jinan, Shandong, Peoples R China
来源
DRUG DISCOVERIES AND THERAPEUTICS | 2014年 / 8卷 / 05期
基金
中国博士后科学基金; 美国国家卫生研究院; 中国国家自然科学基金;
关键词
Epigenetic; HDACs; selective HDACIs; HDAC1/3 selective inhibitors; anti-cancer agent;
D O I
10.5582/ddt.2014.01034
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. inhibitors in clinical settings, further study of their mechanism of anticancer activity and optimization of their structure is warranted.
引用
收藏
页码:225 / 228
页数:4
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