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不同化学结构药物与hERG钾离子通道的相互作用

Diverse drug-hERG potassium channel interactions

  • 摘要: 许多不同化学结构的药物可抑制hERG钾离子通道而引起QT间期延长和心律失常。本文首先介绍hERG钾离子通道在结构和功能上的独特之处,然后总结归纳了典型的具有hERG钾离子通道抑制作用的药物,深入分析其不同的作用模式特点,最后从结构上概括出hERG钾离子通道抑制剂所具有的共同特征,为今后在新化学实体设计中避免心脏不良反应提供有益的帮助。

     

    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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