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α-芋螺毒素(α-CTX)是芋螺毒素的重要家族,由12~19个氨基酸、2~3对二硫键组成,是迄今发现的最小的神经肽类毒素。α-芋螺毒素能特异性地抑制肌肉型或神经元型的烟碱型乙酰胆碱受体(nAChR),并能进一步区分不同的神经元型nAChR亚型。由于其相对分子质量小、活性高,不仅可直接开发为疗效特异的镇痛及抗癫痫等药物,还可作为研究神经生物学工具,鉴定nAChR亚型功能。本文对α-CTX研究的最新进展予以评述,着重介绍了α-CTX的作用靶位特性、构效关系及其应用进展。
Alpha-conotoxin (α-CTX) is an important family of conotoxins, composed of 12 to 19 amino acids, 2 to 3 pairs of disulfide bonds and is by far the smallest neuropeptide toxin found. Alpha-conotoxins specifically inhibit muscle or neuronal nicotinic acetylcholine receptors (nAChRs) and can further differentiate between different neuronal nAChR subtypes. Because of its relatively small molecular mass, high activity, not only can be directly developed for the efficacy of specific analgesic and antiepileptic drugs, but also as a research tool for neurobiology, nAChR subtype identification. In this paper, the latest advances in α-CTX research are reviewed, focusing on the role of α-CTX target characteristics, structure-activity relationship and its application progress.