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电鳐电器官中的受体-离子通道相互作用:巯基修饰的影响

Receptor--ion channel interactions in Torpedo electric organ: influence of thiol group modification.

作者信息

Aronstam R S, Graham J L, Narayanan L

出版信息

Neurosci Lett. 1982 Jul 20;31(1):53-8. doi: 10.1016/0304-3940(82)90053-2.

Abstract

The influence of sulfhydryl and disulfide reagents on nicotinic cholinergic receptors and ion channels and their interactions was investigated using specific probes for receptor and channel binding sites in electric organs from Torpedo californica. N-ethylmaleimide, a sulfhydryl alkylating agent, did not alter receptor or ion channel binding, or receptor-mediated ion channel binding activation or desensitization. Alteration of receptor--ion channel coupling produced by treatment with an organic sulfhydryl, dithiothreitol, could be accounted for on the basis of decreases in receptor affinity for agonists. These changes were reversed by exposure to an oxidizing agent. Following reduction by dithiothreitol, N-ethylmaleimide treatment produced large decreases in the extent and affinity of both receptor and channel binding. No evidence for a direct role of thiol groups in ion channel function was obtained.

摘要

使用针对加州电鳐电器官中受体和通道结合位点的特异性探针,研究了巯基和二硫键试剂对烟碱型胆碱能受体、离子通道及其相互作用的影响。巯基烷基化剂N-乙基马来酰亚胺不会改变受体或离子通道结合,也不会改变受体介导的离子通道结合激活或脱敏。用有机巯基二硫苏糖醇处理导致的受体-离子通道偶联改变,可归因于受体对激动剂亲和力的降低。这些变化通过暴露于氧化剂而逆转。经二硫苏糖醇还原后,N-乙基马来酰亚胺处理使受体和通道结合的程度和亲和力大幅降低。未获得硫醇基团在离子通道功能中直接作用的证据。

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