The human muscarinic M1 acetylcholine receptor, when expressed in CHO cells, activates and downregulates both Gqα and G11α equally and non‐selectively

FEBS Letters

Mullaney, Ian¹  Buckley, Noel J.²  Mitchell, Fiona M.¹  McCallum, J.Fraser¹  Milligan, Graeme¹ 

[1]Molecular Pharmacology Group, Departments of Biochemistry and Pharmacology, University of Glasgow, Glasgow G12 8QQ, Scotland, UK

[2]National Institute for Medical Research, Mill Hill, London NW7 1AA, England, UK

关键词: Guanine nucleotide binding protein;    Phospholipase C;    Inositol trisphosphate;    Muscarinic acetylcholine receptor;   

DOI  :  10.1016/0014-5793(93)81401-K

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

CHO cells express both of the phosphoinositidase C-linked G-proteins G_q and G₁₁ G₁₁α is some 2.5-fold more highly expressed than G_qα 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 G_qα and G_11α. 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 and activates both G_qα and G₁₁α equivalently and non-selectively in a whole cell system in which the receptor has access to both G-proteins.

【 授权许可】

Unknown