Wu Rui-Jie, Wang Lei, Xiang Hui
School of Life Sciences, Sun Yat-Sen University, 132 Outer Ring Road, Guangzhou University City, Guangzhou, Guangdong Province, 510006, People's Republic of China.
Curr Top Med Chem. 2015;16(2):156-69. doi: 10.2174/1568026615666150701114831.
α-Conotoxins (α-Ctxs) are the major class of Ctxs extracted from the venom of marine cone snails. Most α-Ctxs specifically target various subtypes of the nicotinic acetylcholine receptors (nAChRs) with high affinity and potency as antagonists. Therefore, they may be used for the treatment of numerous diseases that nAChRs involved. The subtype affinity and selectivity of α-Ctxs arise from their amino acid composition and geometric conformation of microsites. To reveal the structural features of α-Ctxs, detailed structural information on the various nAChR subtypes and their ligand complexes is needed. This review article provides an overview of the structural data on α-Ctx-nAChR interactions to investigate the prediction and evaluation of the affinity and selectivity of α-Ctx.
α-芋螺毒素(α-Ctxs)是从海洋芋螺毒液中提取的主要一类毒素。大多数α-Ctxs作为拮抗剂,以高亲和力和效力特异性靶向烟碱型乙酰胆碱受体(nAChRs)的各种亚型。因此,它们可用于治疗众多与nAChRs相关的疾病。α-Ctxs的亚型亲和力和选择性源于其氨基酸组成和微位点的几何构象。为了揭示α-Ctxs的结构特征,需要有关各种nAChR亚型及其配体复合物的详细结构信息。本文综述提供了关于α-Ctx-nAChR相互作用的结构数据概述,以研究α-Ctx亲和力和选择性的预测与评估。