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Lead compound optimization strategy (5) - reducing the hERG cardiac toxicity in drug development

文献类型：期刊论文

作者Zhou Shengbin; Wang Jiang; Liu Hong
刊名Acta Pharmaceutica Sinica
出版日期2016
卷号51期号:10页码:1530-1539
关键词hERG lead compound optimization lipophilicity basicity conformation restriction cardiac toxicity
ISSN号0513-4870
其他题名先导化合物结构优化策略(五) 降低药物hERG心脏毒性
文献子类Review
英文摘要The potassium channel encoded by the human ether-a-go-go related gene (hERG) plays a very important role in the physiological and pathological processes in human.hERG potassium channel determines the outward currents which facilitate the repolarization of the myocardial cells.Some drugs were withdrawn from the market for the serious side effect of long QT interval and arrhythmia due to blockade of hERG channel.The strategies for lead compound optimization are to reduce inhibitory activity of hERG potassium channel and decrease cardiac toxicity.These methods include reduction of lipophilicity and basicity of amines, introduction of hydroxyl and acidic groups, and restricting conformation.
资助项目国家杰出青年科学基金资助项目[00000000]
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:5821976
源URL[http://119.78.100.183/handle/2S10ELR8/269232]  
专题药物化学研究室
通讯作者Liu Hong
作者单位Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
推荐引用方式
GB/T 7714		 Zhou Shengbin,Wang Jiang,Liu Hong. Lead compound optimization strategy (5) - reducing the hERG cardiac toxicity in drug development[J]. Acta Pharmaceutica Sinica,2016,51(10):1530-1539.
APA Zhou Shengbin,Wang Jiang,&Liu Hong.(2016).Lead compound optimization strategy (5) - reducing the hERG cardiac toxicity in drug development.Acta Pharmaceutica Sinica,51(10),1530-1539.
MLA Zhou Shengbin,et al."Lead compound optimization strategy (5) - reducing the hERG cardiac toxicity in drug development".Acta Pharmaceutica Sinica 51.10(2016):1530-1539.

入库方式： OAI收割

来源：上海药物研究所

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