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首页> 外文期刊>Expert opinion on therapeutic targets >The hERG potassium channel as a therapeutic target.
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The hERG potassium channel as a therapeutic target.

机译：hERG钾通道作为治疗靶标。

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摘要

The hERG (human ether-a-go-go-related gene) potassium channel has elicited intense scientific interest due to its counter-intuitive kinetics and its association with arrhythmia and sudden death. hERG blockade is involved in both antiarrhythmic pharmacotherapy and the pathogenesis of familial and acquired long QT syndrome (LQTS). Short QT syndrome (SQTS), muscular atrophy and many forms of cancer have also been associated with hERG as a target. Molecular models of both the channel and its blocker pharmacophores exist, revealing methods to design hERG liability out of potential drug molecules. Future developments will synthesise preclinical data on hERG with other criteria to determine net arrhythmogenic risk. Also, the molecular actions of hERG and its genetics will be elucidated in detail to allow clinical risk reduction.
机译：hERG（与人类醚相关的基因）钾通道因其反直觉的动力学以及与心律不齐和猝死的关系而引起了强烈的科学兴趣。 hERG阻滞参与抗心律失常药物治疗以及家族性和获得性长QT综合征（LQTS）的发病机理。短QT综合征（SQTS），肌肉萎缩和许多形式的癌症也已与hERG作为靶标相关联。该通道及其阻断剂药效团的分子模型均存在，揭示了从潜在药物分子中设计hERG责任的方法。未来的发展将综合hERG的临床前数据与其他标准，以确定净心律失常风险。同样，将详细阐明hERG的分子作用及其遗传学，以降低临床风险。

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