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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.

DOI:10.1002/j.1460-2075.1986.tb04431.x
PMID:3758027
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1167045/
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
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/797e/1167045/810e47c96eef/emboj00171-0084-a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/797e/1167045/810e47c96eef/emboj00171-0084-a.jpg

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本文引用的文献

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Primary structures of beta- and delta-subunit precursors of Torpedo californica acetylcholine receptor deduced from cDNA sequences.从cDNA序列推导的加州电鳐乙酰胆碱受体β和δ亚基前体的一级结构。
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Covalent labeling of the acetylcholine receptor from Torpedo electric tissue with the channel blocker [3H]triphenylmethylphosphonium by ultraviolet irradiation.
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Determinants of phencyclidine potency on the nicotinic acetylcholine receptors from muscle and electric organ.苯环利定对肌肉和电鳐电器官烟碱型乙酰胆碱受体作用强度的决定因素。
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Mutations in the M1 region of the nicotinic acetylcholine receptor alter the sensitivity to inhibition by quinacrine.烟碱型乙酰胆碱受体M1区域的突变改变了对奎纳克林抑制作用的敏感性。
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Acetylcholine receptor and ion conductance modulator sites at the murine neuromuscular junction: evidence from specific toxin reactions.小鼠神经肌肉接头处的乙酰胆碱受体和离子电导调节位点：来自特定毒素反应的证据。
Proc Natl Acad Sci U S A. 1973 Mar;70(3):949-53. doi: 10.1073/pnas.70.3.949.
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Eur J Biochem. 1985 Mar 15;147(3):483-7. doi: 10.1111/j.0014-2956.1985.00483.x.
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Studies on the effect of histrionicotoxin on the monocellular electroplax from Electrophorus electricus and on the binding of (3H)acetylcholine to membrane fragments from Torpedo marmorata.关于组织胺毒素对电鳗单细胞膜片以及对（3H）乙酰胆碱与电鳐膜碎片结合作用的研究。
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Membranes rich in acetylcholine receptor: characterization and reconstitution to excitable membranes from exogenous lipids.富含乙酰胆碱受体的膜：特性及从外源脂质重构为可兴奋膜。
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