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Conotoxins: Structure, Therapeutic Potential and Pharmacological Applications

机译:芋螺毒素:结构,治疗潜力和药理学应用

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摘要

Cone snails, also known as marine gastropods, from Conus genus produce in their venom a diverse range of small pharmacologically active structured peptides called conotoxins. The cone snail venoms are widely unexplored arsenal of toxins with therapeutic and pharmacological potential, making them a treasure trove of ligands and peptidic drug leads. Conotoxins are small disulfide bonded peptides, which act as remarkable selective inhibitors and modulators of ion channels (calcium, sodium, potassium), nicotinic acetylcholine receptors, noradrenaline transporters, N-methyl-D-aspartate receptors, and neurotensin receptors. They are highly potent and specific against several neuronal targets making them valuable as research tools, drug leads and even therapeutics. In this review, we discuss their gene superfamily classification, nomenclature, post-translational modification, structural framework, pharmacology and medical applications of the active conopeptides. We aim to give an overview of their structure and therapeutic potential. Understanding these aspects of conopeptides will help in designing more specific peptidic analogues.
机译:来自圆锥属的锥蜗牛,也称为海洋腹足类动物,在其毒液中产生各种各样的称为药毒素的小药理活性结构化肽。锥蜗牛毒是尚未广泛开发的具有治疗和药理潜力的毒素武库,使其成为配体和肽类药物前导的宝库。芋螺毒素是小的二硫键肽,可作为离子通道(钙,钠,钾),烟碱乙酰胆碱受体,去甲肾上腺素转运蛋白,N-甲基-D-天冬氨酸受体和神经降压素受体的显着选择性抑制剂和调节剂。它们非常有效并且针对几种神经元靶标,使其具有重要的研究工具,药物线索甚至治疗方法的价值。在这篇综述中,我们讨论了它们的基因超家族分类,命名法,翻译后修饰,结构框架,药理学和活性肽的医学应用。我们旨在概述其结构和治疗潜力。了解肽段的这些方面将有助于设计更具体的肽类似物。

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