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人毒蕈碱型M1乙酰胆碱受体在CHO细胞中表达时,会同等且非选择性地激活和下调Gqα和G11α。

The human muscarinic M1 acetylcholine receptor, when express in CHO cells, activates and downregulates both Gq alpha and G11 alpha equally and non-selectively.

作者信息

Mullaney I, Mitchell F M, McCallum J F, Buckley N J, Milligan G

机构信息

Department of Biochemistry, University of Glasgow, Scotland, UK.

出版信息

FEBS Lett. 1993 Jun 14;324(2):241-5. doi: 10.1016/0014-5793(93)81401-k.

Abstract

CHO cells express both of the phosphoinositidase C-linked G-proteins Gq and G11. G11 alpha is some 2.5-fold more highly expressed than Gq alpha in membranes of these cells. Following transfection and stable expression of CHO cells with DNA encoding the human muscarinic M1 acetylcholine (HM1) receptor, chronic treatment of the cells with the cholinergic agonist carbachol resulted in down-regulation of membrane levels of both Gq alpha and G11 alpha. Dose-response curves to carbachol produced identical EC50 values for agonist-induced down-regulation of the two G-proteins and both were down-regulated with the same time course. These data indicate that the HM1 receptor interacts with the activates both Gq alpha and G11 alpha equivalently and non-selectively in a whole cell system in which the receptor has access to both G-proteins.

摘要

CHO细胞表达与磷酸肌醇酶C相连的G蛋白Gq和G11。在这些细胞的膜中,G11α的表达量比Gqα高约2.5倍。用编码人毒蕈碱型M1乙酰胆碱(HM1)受体的DNA转染CHO细胞并使其稳定表达后,用胆碱能激动剂卡巴胆碱对细胞进行长期处理,导致Gqα和G11α的膜水平下调。卡巴胆碱的剂量反应曲线显示,激动剂诱导的两种G蛋白下调产生相同的EC50值,且两者在相同的时间进程中被下调。这些数据表明,在受体能够接触到两种G蛋白的全细胞系统中,HM1受体与Gqα和G11α等效且非选择性地相互作用并激活它们。

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