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channel determines the outward currents which facilitate the repolarization of the myocardial cells.Some drugs were withdrawn from the market for the serious side effect of long QT interval and arrhythmia due to blockade of hERG channel.The strategies for lead compound optimization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. |
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