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芋螺中烟碱型乙酰胆碱受体调节剂

Neuronal Nicotinic Acetylcholine Receptor Modulators from Cone Snails.

机构信息

IMB Centre for Pain Research, Institute for Molecular Bioscience, The University of Queensland, St. Lucia, QLD 4072, Australia.

出版信息

Mar Drugs. 2018 Jun 13;16(6):208. doi: 10.3390/md16060208.

Abstract

Marine cone snails are a large family of gastropods that have evolved highly potent venoms for predation and defense. The cone snail venom has exceptional molecular diversity in neuropharmacologically active compounds, targeting a range of receptors, ion channels, and transporters. These conotoxins have helped to dissect the structure and function of many of these therapeutically significant targets in the central and peripheral nervous systems, as well as unravelling the complex cellular mechanisms modulated by these receptors and ion channels. This review provides an overview of α-conotoxins targeting neuronal nicotinic acetylcholine receptors. The structure and activity of both classical and non-classical α-conotoxins are discussed, along with their contributions towards understanding nicotinic acetylcholine receptor (nAChR) structure and function.

摘要

海洋圆锥蜗牛是腹足纲的一个大家族,它们进化出了高效的毒液用于捕食和防御。圆锥蜗牛毒液具有出色的分子多样性,其中包含许多具有神经药理学活性的化合物,靶向一系列受体、离子通道和转运体。这些芋螺毒素有助于解析中枢和外周神经系统中许多具有治疗意义的靶标结构和功能,以及揭示这些受体和离子通道调节的复杂细胞机制。本综述概述了作用于神经元烟碱型乙酰胆碱受体的α-芋螺毒素。讨论了经典和非经典α-芋螺毒素的结构和活性,以及它们对理解烟碱型乙酰胆碱受体(nAChR)结构和功能的贡献。

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