期刊文献+

药物与hERG钾通道相互作用预测的研究进展 被引量:4

In silico prediction of drug-hERG potassium channel interaction
下载PDF
导出
摘要 不少药物因临床发现有抑制hERG钾离子通道导致心律失常而被撤出市场,本文从hERG钾通道的生物学基础,阻断hERG钾离子通道的高危险性及采用计算机虚拟预测药物对hERG钾离子通道阻滞活性的研究方法分别进行了介绍和综述,并分别从基于受体和基于配体两个角度对各种预测药物阻滞hERG钾离子通道活性的方法的研究进行阐述和比较。 Many drugs were withdrawn from the market due to its serious side-effects such as cardiotoxicity after blocking hERG potassium channel. The biological characteristics of hERG potassium channel, high risks resulting from blocking this channel and in silico prediction of the interaction between drugs and hERG potassium channel are presented in this review. Efforts are made to characterize andaccount for the different characteristics and objectives of various in silico approaches, including receptor-based, and ligand-based approaches.
出处 《中国药科大学学报》 CAS CSCD 北大核心 2006年第4期291-296,共6页 Journal of China Pharmaceutical University
关键词 hFRG 钾离子通道 基于受体的阻滞活性预测 基于配体的阻滞活性预测 hERG potassium channel receptor-based prediction ligand-based prediction
  • 相关文献

二级参考文献62

  • 1Sanguinetti MC, Jurkiewicz NK. Two components of cardiac delayed rectifier K^+ current: differential sensitivity to block by class Ⅲ antiarrhythmic agents. J Gen Physiol 1990;96: 195-215.
  • 2Varro A, Balati B, Iost N, Takacs J, Virag L, Lathrop DA, et al.The role of the delayed rectifier component IKs in dog ventricular muscle and Purkinje fiber repolarization. J Physiol 2000; 523: 67-81.
  • 3Cheng J, Kamiya K, Liu W, Tsuji Y, Toyama J, Kodama I.Heterogeneous distribution of the two components of delayed rectifier K^+ current: a potential mechanism of the proarrhythmic effects of methanesulfonanilide class Ⅲ agents.Cardiovasc Res 1999; 43: 135-47.
  • 4Roden DM, Balser JR, George Jr AL, Anderson ME. Cardiac ion channels. Annu Rev Physiol 2002; 64:431-75.
  • 5Virag L, Iost N, Opincariu M, Szolnoky J, Szecsi J, Bogats G, et al. The slow component of the delayed rectifier potassium current in undiseased human ventricular myocytes.Cardiovasc Res 2001.40. 700-7.
  • 6Iost N, Virag L, Opincariu M, Szecsi J, Varro A, Papp JG.Delayed rectifier potassium current in undiseased human ventricular myocytes. Cardiovasc Res 1998; 40: 508-15.
  • 7Xu X, Rials S J, Wu Y, Salata JJ, Liu T, Bharucha DB, et al.Left ventricular hypertrophy decreases slowly but not rapidly activating delayed rectifier potassium currents of epicardial and endocardial myocytes in rabbits. Circulation 2001;103: 1585-90.
  • 8Lengyel C, Iost N, Virag L, Varro A, Lathrop DA, Papp JG.Pharmacological block of the slow component of the outward delayed rectifier current (IKs) fails to lengthen rabbit ventricular muscle QTc and action potential duration. Br J Pharmacol 2001; 132: 101-10.
  • 9Lu Z, Kamiya K, Opthof T, Yasui K, Kodama I. Density and kinetics of IKr and IKs in guinea pig and rabbit ventricular myocytes explain different efficacy of IKs blockade at high heart rate in guinea pig and rabbit: implications for arrhythmogenesis in humans. Circulation 2001; 104:951-6.
  • 10Gintant GA. Two components of delayed rectifier current in canine atrium and ventricle. Does IKs play a role in the reverse rate dependence of class Ⅲ agents? Circ Res 1996; 78: 26-37.

共引文献9

同被引文献47

引证文献4

二级引证文献29

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部