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

	Lead compound optimization strategy (5) - reducing the hERG cardiac toxicity in drug development
	Zhou Shengbin; Wang Jiang; Liu Hong
刊名	Acta Pharmaceutica Sinica
	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channel determines the outward currents which facilitate the repolarization of the myocardial cells.Some drugs were withdrawn from the market for the serious side effect of long QT interval and arrhythmia due to blockade of hERG channel.The strategies for lead compound optimization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
内容类型	期刊论文
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.