作用于烟碱乙酰胆碱受体的α*-芋螺毒素研究进展

被引:3
作者
徐盼 [1 ,2 ]
吴勇 [1 ,3 ]
邴晖 [1 ,3 ]
长孙东亭 [1 ,3 ]
罗素兰 [1 ,3 ]
机构
[1] 海南大学热带生物资源教育部重点实验室海口市海洋药物重点实验室
[2] 海南大学农学院
[3] 海南大学海洋学院
关键词
生物活性肽; α*-芋螺毒素(α*-CTx); 烟碱型乙酰胆碱受体(nAChR); 构效关系;
D O I
10.16605/j.cnki.1007-7847.2017.01.016
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
芋螺毒素(conotoxin,conopeptide,CTx)是由热带海洋中的肉食性软体动物芋螺分泌产生的一大类生物活性肽,它们相对分子质量小,能特异地作用于动物体内各种离子通道和受体,具有巨大的药物开发价值。其中,A-超家族的α-芋螺毒素(α-CTx)是发现最早的且最重要的一类成员,它能特异性作用于烟碱型乙酰胆碱受体(nicotinic acetylcholine receptors,nAChRs),是肌肉或神经型nAChRs的选择性阻断剂。nAChRs与中枢神经系统紊乱如疼痛、成瘾、癌症等多种疾病密切相关。近年来,人们陆续发现其他超家族的芋螺毒素中也有成员可阻断nAChRs,如αA-、αB-、αO-、αC-、αD-、αS-等家族的芋螺毒素。上述能阻断nAChRs的芋螺毒素统称为α*-芋螺毒素(α*-CTx)。α*-芋螺毒素对nAChRs阻断活性的差别与它们的结构有着密切的联系。结合国内外研究现状,对α*-CTx与nAChRs相互作用的关键位点以及结构与功能的关系进行综述,可为相关研究提供参考。
引用
收藏
页码:85 / 94
页数:10
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