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Diverse drug-hERG potassium channel interactions

Yadong Chen

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Abstract

Many agents with diverse chemical structures and therapeutic classes could inhibit hERG potassium channel,and could then cause prolongation of the QT interval and arrhythmia.Herein,the particular characteristics of hERG potassium channel were described,and the representative hERG potassium channel inhibitors were collected.Accordingly,the interaction modes of diverse agents and hERG potassium channel were analyzed;the common structural features of hERG potassium channel inhibitors were summarized;and some advice on how to avoid hERG inhibitory liability and the following cardiac risk in design and optimization of new chemical entity were proposed.

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What this paper is about

Many agents with diverse chemical structures and therapeutic classes could inhibit hERG potassium channel,and could then cause prolongation of the QT interval and arrhythmia.Herein,the particular characteristics of hERG potassium channel were described,and the representative hERG potassium channel inhibitors were collected.Accordingly,the interaction modes of diverse agents and hERG potassium channel were analyzed;the common structural features of hERG potassium channel inhibitors were summarized;and some advice on how to avoid hERG inhibitory liability and the following cardiac risk in design and optimization of new chemical entity were proposed.

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Available abstract

Many agents with diverse chemical structures and therapeutic classes could inhibit hERG potassium channel,and could then cause prolongation of the QT interval and arrhythmia.Herein,the particular characteristics of hERG potassium channel were described,and the representative hERG potassium channel inhibitors were collected.Accordingly,the interaction modes of diverse agents and hERG potassium channel were analyzed;the common structural features of hERG potassium channel inhibitors were summarized;and some advice on how to avoid hERG inhibitory liability and the following cardiac risk in design and optimization of new chemical entity were proposed.

Key concepts: hERG, Potassium channel, Pharmacology, Potassium channel blocker, Chemistry, Drug, Potassium, QT interval

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