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烟碱型乙酰胆碱受体δ亚基中非竞争性拮抗剂的反应位点。

The reaction site of a non-competitive antagonist in the delta-subunit of the nicotinic acetylcholine receptor.

作者信息

Oberthür W, Muhn P, Baumann H, Lottspeich F, Wittmann-Liebold B, Hucho F

出版信息

EMBO J. 1986 Aug;5(8):1815-9. doi: 10.1002/j.1460-2075.1986.tb04431.x.

Abstract

A site in the primary structure of the nicotinic acetylcholine receptor from Torpedo marmorata covalently labeled with the non-competitive antagonist [3H]triphenylmethylphosphonium (TPMP+) was localized. The label was found in position 262 of the delta-polypeptide chain. This site is specifically labeled in the presence of the agonist carbamoylcholine. Labeling is prevented by the non-competitive antagonist histrionicotoxin. Position 262, probably a serine, is located in the highly conserved membrane-spanning helix M2 (according to the predicted folding scheme of Finer-Moore and Stroud (1984). The relationship of this site to the receptor's ion channel and its regulation is discussed.

摘要

定位了来自电鳐的烟碱型乙酰胆碱受体一级结构中一个与非竞争性拮抗剂[³H]三苯甲基鏻(TPMP⁺)共价标记的位点。该标记位于δ-多肽链的第262位。在激动剂氨甲酰胆碱存在的情况下,此位点会被特异性标记。非竞争性拮抗剂组蛋白毒素可阻止标记。第262位可能是丝氨酸,位于高度保守的跨膜螺旋M2中(根据Finer-Moore和Stroud(1984年)预测的折叠方案)。讨论了该位点与受体离子通道及其调节的关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/797e/1167045/810e47c96eef/emboj00171-0084-a.jpg

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