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蝎子和蜘蛛毒液中与疼痛相关的毒素:直面离子通道

Pain-related toxins in scorpion and spider venoms: a face to face with ion channels.

作者信息

Diochot Sylvie

机构信息

Institut de Pharmacologie Moléculaire et Cellulaire (IPMC), Centre National de la Recherche Scientifique (CNRS) UMR 7275 et Université Côte d'Azur (UCA), 06560 Valbonne, France. Institut de Pharmacologie Moléculaire et Cellulaire Centre National de la Recherche Scientifique Université Côte d'Azur Valbonne France.

出版信息

J Venom Anim Toxins Incl Trop Dis. 2021 Dec 6;27:e20210026. doi: 10.1590/1678-9199-JVATITD-2021-0026. eCollection 2021.

Abstract

Pain is a common symptom induced during envenomation by spiders and scorpions. Toxins isolated from their venom have become essential tools for studying the functioning and physiopathological role of ion channels, as they modulate their activity. In particular, toxins that induce pain relief effects can serve as a molecular basis for the development of future analgesics in humans. This review provides a summary of the different scorpion and spider toxins that directly interact with pain-related ion channels, with inhibitory or stimulatory effects. Some of these toxins were shown to affect pain modalities in different animal models providing information on the role played by these channels in the pain process. The close interaction of certain gating-modifier toxins with membrane phospholipids close to ion channels is examined along with molecular approaches to improve selectivity, affinity or bioavailability for therapeutic purposes.

摘要

疼痛是蜘蛛和蝎子毒液注入时引发的常见症状。从它们的毒液中分离出的毒素已成为研究离子通道功能和生理病理作用的重要工具,因为这些毒素能调节离子通道的活性。特别是那些具有止痛效果的毒素,可作为未来人类镇痛药研发的分子基础。本综述总结了不同的蝎子和蜘蛛毒素,它们直接与疼痛相关的离子通道相互作用,具有抑制或刺激作用。其中一些毒素已被证明会影响不同动物模型中的疼痛模式,从而提供这些通道在疼痛过程中所起作用的相关信息。同时还探讨了某些门控修饰毒素与离子通道附近膜磷脂的紧密相互作用,以及为治疗目的提高选择性、亲和力或生物利用度的分子方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4d59/8667759/0d504b3a4dcf/1678-9199-jvatitd-27-e20210026-gf1.jpg

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