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加州电鳐烟碱型乙酰胆碱受体中α-芋螺毒素与蛇毒神经毒素结合位点之间的关系。

Relationship between the binding sites for an alpha-conotoxin and snake venom neurotoxins in the nicotinic acetylcholine receptor from Torpedo californica.

作者信息

Utkin Y N, Kobayashi Y, Hucho F, Tsetlin V I

机构信息

Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences.

出版信息

Toxicon. 1994 Sep;32(9):1153-7. doi: 10.1016/0041-0101(94)90399-9.

Abstract

Photoinduced cross-links between the iodinated Lys26-p-azidobenzoyl derivative of neurotoxin II from Naja naja oxiana cobra venom and nicotinic acetylcholine receptor from Torpedo californica (AChR) have been studied in the presence of alpha-conotoxin GI from the marine snail C. geographus. Preincubation of the AChR-enriched membranes with increasing concentrations of alpha-conotoxin GI protects first the gamma subunit from photolabelling and then the delta subunit, the IC50 values being 0.76 and 5.01 microM, respectively. The results obtained, in view of the relevant data in literature, demonstrate that the (alpha + gamma) site, which is the high affinity site for d-tubocurarine, has also a higher affinity for an alpha-conotoxin than the (alpha + delta) containing site. The latter has a somewhat higher affinity than the (alpha + gamma) site towards some naturally occurring snake venom alpha-neurotoxins or their derivatives.

摘要

在来自地纹芋螺的α-芋螺毒素GI存在的情况下,研究了来自中亚眼镜蛇毒的神经毒素II的碘化赖氨酸26 - 对叠氮苯甲酰衍生物与加州电鳐烟碱型乙酰胆碱受体(AChR)之间的光诱导交联。用浓度递增的α-芋螺毒素GI对富含AChR的膜进行预孵育,首先保护γ亚基不被光标记,然后保护δ亚基,IC50值分别为0.76和5.01微摩尔。鉴于文献中的相关数据,所得结果表明,作为d - 筒箭毒碱高亲和力位点的(α + γ)位点,对α-芋螺毒素的亲和力也高于含(α + δ)的位点。后者对一些天然存在的蛇毒α-神经毒素或其衍生物的亲和力略高于(α + γ)位点。

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