| 药物对hERG钾通道作用机制研究进展 |
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| 引用本文： | 林敏,李泱,张建成.药物对hERG钾通道作用机制研究进展[J].中国药理学与毒理学杂志,2012,26(4):581-584. |
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| 作者姓名： | 林敏 李泱 张建成 |
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| 作者单位： | 1. 福建医科大学省立临床学院,福建福州,350001
2. 解放军总医院老年心血管病研究所,北京,100853 |
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| 基金项目： | 国家自然科学基金资助项目 |
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| 摘 要： | 人ether-a-go-go-related gene(hERG)钾通道表达了延迟整流钾电流的快激活成分,对动作电位的复极至关重要。hERG钾电流不仅是抗心律失常作用的主要靶点,也是诸多药物增加尖端扭转型室速和心源性猝死风险的关键位点,而该电流的降低和(或)升高与基因突变或药物阻滞作用密切相关。随着对药物与hERG钾通道相互作用机制研究的深入,药物与通道孔道区蛋白结合位点的作用及其对通道转运的影响逐步被揭示,但这些药物对hERG作用的临床应用仍有待评价。
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| 关 键 词： | hERG 药物反应 通道转运 钾通道 |
| 收稿时间： | 2011-9-2 |
| 修稿时间： | 2012-2-9 |
Research progress in drug reactions on hERG potassium channels |
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| LIN Min
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LI Yang
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ZHANG Jian-cheng.Research progress in drug reactions on hERG potassium channels[J].Chinese Journal of Pharmacology and Toxicology,2012,26(4):581-584. |
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| Authors: | LIN Min LI Yang ZHANG Jian-cheng |
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| Institution: | 1. Provincial Clinical Medicine College of Fujian Medical University, Fuzhou 350001, China;2. Institute of Geriatric Cardiology of Chinese PLA General Hospital, Beijing 100853, China |
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| Abstract: | Human ether-a-go-go-related gene (hERG) potassium channels conduct the rapid component of the delayed rectifier potassium current (IKr). The reduction (or increase) of IKr current due to either gene mutations or adverse drug effects would increase the risk of torsades de pointes and sudden cardiac death. This paper reviews various mechanisms of drug reactions of hERG potassium channels and the properties of major drug-protein reaction sites in the pore region and trafficking of hERG potassium channels under the influence of drugs. However, the effect of clinical administration of drugs on hERG remains unclear. |
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| Keywords: | hERG adverse drug reaction channels trafficking potassium channels |
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