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源自蝎毒的Shal型(Kv4)钾通道孔区阻断剂

Pierre Edouard Bougis^*, Marie-France Martin-Eauclaire

艾克斯-马赛大学，法国国家科学研究中心，马赛神经生物学和神经生理学研究中心UMR7286，马赛 13344，法国

摘要

KCND/Kv4 (Shal)家族成员负责编码电压门控钾通道(Kv4.1, Kv4.2和Kv4.3)，这类通道在心脏和神经元中调节自然和快速失活的A型钾电流。该A型钾电流可被隶属于α钾通道毒素第15家族的短链蝎神经毒素特异性地抑制。这类毒素也被称为孔区阻断剂，与调节通道门控特征的蜘蛛毒素的作用模式是不同的。本文综述了α钾通道毒素第15家族的化学及药理学信息。

关键词： 钾通道; 电压门控钾通道第4家族; 孔区阻断剂; 蝎毒

分类号：Q965.9;Q74

Shal-type (Kv4.x) potassium channel pore blockers from scorpion venoms

Pierre Edouard Bougis^*, Marie-France Martin-Eauclaire

Aix-Marseille University, The National Center for Scientific Research (CNRS), Research Center for Neurobiology and Neurophysiology of Marseille UMR7286, 13344, Marseille, France

Abstract

Voltage-gated potassium channels (Kv4.1, Kv4.2 and Kv4.3) encoded by the members of the KCND/Kv4 (Shal) channel family mediate the native, fast inactivating (A-type) K+ current (IA) described both in heart and neurons. This IA current is specifically blocked by short scorpion toxins that belong to the α-KTx15 subfamily and which act as pore blockers, a different mode of action by comparison to spider toxins known as gating modifiers. This review summarizes our present chemical and pharmacological knowledge on the α-KTx15 toxins.

Key words: Potassium channel; Kv4; pore blockers; scorpion venoms

收稿日期：2015-02-24　　录用日期：2015-05-25

通讯作者：Pierre Edouard Bougis　　E-mail: pierre-edouard.bougis@univ-amu.fr

引用本文：

Pierre Edouard Bougis, Marie-France Martin-Eauclaire. 源自蝎毒的Shal型(Kv4)钾通道孔区阻断剂[J]. 生理学报 2015; 67 (3): 248-254.

Pierre Edouard Bougis, Marie-France Martin-Eauclaire. Shal-type (Kv4.x) potassium channel pore blockers from scorpion venoms. Acta Physiol Sin 2015; 67 (3): 248-254 (in Chinese with English abstract).