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蝎毒素肽在离子通道亚基水平上的作用。

Scorpion toxin peptide action at the ion channel subunit level.

机构信息

College of Medicine and Dentistry, Cairns Campus, James Cook University, Cairns, Queensland 4878, Australia; Translational Neuroscience Facility and Department of Physiology, School of Medical Sciences, UNSW Australia, Sydney, NSW 2052, Australia.

Translational Neuroscience Facility and Department of Physiology, School of Medical Sciences, UNSW Australia, Sydney, NSW 2052, Australia.

出版信息

Neuropharmacology. 2017 Dec;127:46-78. doi: 10.1016/j.neuropharm.2016.10.004. Epub 2016 Oct 10.

Abstract

This review categorizes functionally validated actions of defined scorpion toxin (SCTX) neuropeptides across ion channel subclasses, highlighting key trends in this rapidly evolving field. Scorpion envenomation is a common event in many tropical and subtropical countries, with neuropharmacological actions, particularly autonomic nervous system modulation, causing significant mortality. The primary active agents within scorpion venoms are a diverse group of small neuropeptides that elicit specific potent actions across a wide range of ion channel classes. The identification and functional characterisation of these SCTX peptides has tremendous potential for development of novel pharmaceuticals that advance knowledge of ion channels and establish lead compounds for treatment of excitable tissue disorders. This review delineates the unique specificities of 320 individual SCTX peptides that collectively act on 41 ion channel subclasses. Thus the SCTX research field has significant translational implications for pathophysiology spanning neurotransmission, neurohumoral signalling, sensori-motor systems and excitation-contraction coupling. This article is part of the Special Issue entitled 'Venom-derived Peptides as Pharmacological Tools.'

摘要

这篇综述对已鉴定的蝎子毒素 (SCTX) 神经肽在离子通道亚类中的功能验证作用进行了分类,突出了这一快速发展领域的主要趋势。蝎子蜇伤在许多热带和亚热带国家很常见,具有神经药理学作用,特别是自主神经系统调节,导致高死亡率。蝎子毒液中的主要活性成分是一组多样化的小分子神经肽,它们在广泛的离子通道类别中引起特定的强效作用。这些 SCTX 肽的鉴定和功能特征对于开发新型药物具有巨大的潜力,可以提高对离子通道的认识,并为治疗兴奋组织疾病建立先导化合物。本综述描述了 320 种单独的 SCTX 肽的独特特异性,它们共同作用于 41 种离子通道亚类。因此,SCTX 研究领域对神经传递、神经激素信号、感觉-运动系统和兴奋-收缩偶联等方面的病理生理学具有重要的转化意义。本文是题为“毒液衍生肽作为药理学工具”的特刊的一部分。

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