摘要
最近研究表明hERG(human ether-a—go-go related gene)基因编码的钾离子通道(hERG通道)作为一种广谱的药物靶标,被某些药物作用时会引起长QT间期综合征(LQTS),甚至导致具有生命危险的室性心律失常——尖端扭转性室性心动过速(TdP),引起制药公司和安全部门的广泛关注,现就hERG通道的结构和功能特征、不同亚基及细胞环境对其调节、目前临床前体内体外的研究方法及关于hERG通道的药物安全性评价进行简要介绍。
More recent studies have shown that the K ^＋ channel encoded by the human ether-a- go-go related gene（hERG） as the molecular target for a wide range of drugs is associated with long-QT syndrome（LQTS） even a life-threatening form of arrhythmia known as Torsade de Points. This is major pharmacological safety concern faced by the pharmaceutical industry and the health regulation authorities. This review is about the following topics ： structure and function of hERG channels ; hERG channel modulation by different β subunits and cellular milieu; contemporary preclinical in vitro and in vivo methods about hERG channel and drug safety evaluation and research.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2007年第12期912-917,共6页
Chinese Journal of New Drugs
基金
国家"863"计划资助项目(2002AA22342D)
