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Research ArticleArticle

Activation of Guanosine 5′-[γ-35S]thio-triphosphate Binding through M1 Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 1. Mathematical Analysis of Catalytic G Protein Activation

Magali Waelbroeck
Molecular Pharmacology April 2001, 59 (4) 875-885; DOI: https://doi.org/10.1124/mol.59.4.875
Magali Waelbroeck
Department of Biochemistry and Nutrition, Medical School, Université Libre de Bruxelles, Brussels, Belgium
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Abstract

I analyzed in this work the effect of agonists and unlabeled guanyl nucleotides on [35S]GTPγS and [3H]NMS binding to transfected CHO cells expressing hM1 muscarinic receptors. I was unable to explain my kinetic results by “traditional” (one-site, two-site, or two-step) bimolecular binding models. I therefore examined the equations that describe catalytic G protein activation. My results were fully consistent with the following interpretation: G protein-coupled receptors either interacted with GDP-bound G proteins and facilitated the GDP release or recognized empty G proteins, depending on the incubation conditions. The receptor-coupled empty G proteins (RG) then recognized GTPγS, and the occupied G protein (G GTPγS* ) dissociated reversibly from the receptor. Agonists accelerated the GDP release from receptor-coupled G proteins and accelerated theG GTPγS* dissociation: both effects accelerated synergically the G protein-GTPγS association reaction in the presence of GDP. GTPγS-bound G proteins,G GTPγS* , competed efficiently with inactive (empty or GDP-bound) G proteins for receptor recognition, and were able, therefore, at low concentrations, to quench the [35S]GTPγS binding reaction.

Footnotes

    • Received August 8, 2000.
    • Accepted January 9, 2001.
  • Send reprint requests to: Dr. Waelbroeck, Laboratoire de Chimie Biologique et de la Nutrition, Faculté de Médecine de l'Université Libre de Bruxelles, Bât. G/E, CP 611, 808 Route de Lennik, B–1070 Brussels, Belgium. E-mail:mawaelbr{at}ulb.ac.be

  • Supported by Grant 3.4504.99 from the Fonds de la Recherche Scientifique Médicale, by an “Action de Recherche Concertée” from the “Communauté Française de Belgique” and by a “Interuniversity Poles of Attraction Program - Belgian State, Prime Minister's Office - Federal Office for Scientific, Technical and Cultural Affairs”.

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Molecular Pharmacology: 59 (4)
Molecular Pharmacology
Vol. 59, Issue 4
1 Apr 2001
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Research ArticleArticle

Activation of Guanosine 5′-[γ-35S]thio-triphosphate Binding through M1 Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 1. Mathematical Analysis of Catalytic G Protein Activation

Magali Waelbroeck
Molecular Pharmacology April 1, 2001, 59 (4) 875-885; DOI: https://doi.org/10.1124/mol.59.4.875

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Research ArticleArticle

Activation of Guanosine 5′-[γ-35S]thio-triphosphate Binding through M1 Muscarinic Receptors in Transfected Chinese Hamster Ovary Cell Membranes: 1. Mathematical Analysis of Catalytic G Protein Activation

Magali Waelbroeck
Molecular Pharmacology April 1, 2001, 59 (4) 875-885; DOI: https://doi.org/10.1124/mol.59.4.875
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