ArticleBritish journal of pharmacology2001
G(q/11) and G(i/o) activation profiles in CHO cells expressing human muscarinic acetylcholine receptors: dependence on agonist as well as receptor-subtype.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
26 citing papers in PubMed, 85 citations in OpenAlex.
- β-arrestin recruitment facilitates a direct association with G proteins.Nature communications · 2026Article
- The M3 Muscarinic Acetylcholine Receptor Can Signal through Multiple G Protein Families.Molecular pharmacology · 2024Article
- Agonist-selective activation of individual G-proteins by muscarinic receptors.Scientific reports · 2024Article
- The Impact of Neurotransmitters on the Neurobiology of Neurodegenerative Diseases.International journal of molecular sciences · 2023Review
- Functional activation of GαJournal of neural transmission (Vienna, Austria : 1996) · 2017Article
- Cholinergic modulation of the hippocampal region and memory function.Journal of neurochemistry · 2017Review
- Cyclophosphamide-induced HCN1 channel upregulation in interstitial Cajal-like cells leads to bladder hyperactivity in mice.Experimental & molecular medicine · 2017Article
- A New Generation of FRET Sensors for Robust Measurement of Gαi1, Gαi2 and Gαi3 Activation Kinetics in Single Cells.PloS one · 2016Article
- Novel structural and functional insights into M3 muscarinic receptor dimer/oligomer formation.The Journal of biological chemistry · 2013Article
- Regulation of neuronal plasticity and fear by a dynamic change in PAR1-G protein coupling in the amygdala.Molecular psychiatry · 2013Article
- The KDEL receptor couples to Gαq/11 to activate Src kinases and regulate transport through the Golgi.The EMBO journal · 2012Article
- Structural aspects of M₃ muscarinic acetylcholine receptor dimer formation and activation.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
- Allosteric modulation of the M₃ muscarinic receptor by amiodarone and N-ethylamiodarone: application of the four-ligand allosteric two-state model.Molecular pharmacology · 2011Article
- Use of the GTPγS ([35S]GTPγS and Eu-GTPγS) binding assay for analysis of ligand potency and efficacy at G protein-coupled receptors.British journal of pharmacology · 2010Review
- Comparative effects of the endogenous agonist glucagon-like peptide-1 (GLP-1)-(7-36) amide and the small-molecule ago-allosteric agent "compound 2" at the GLP-1 receptor.The Journal of pharmacology and experimental therapeutics · 2010Article
- Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.Current opinion in drug discovery & development · 2010Review
- Na/H exchanger regulatory factors control parathyroid hormone receptor signaling by facilitating differential activation of G(alpha) protein subunits.The Journal of biological chemistry · 2010Article
- Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.Pharmacological reviews · 2010Review
- Stereochemistry of an agonist determines coupling preference of beta2-adrenoceptor to different G proteins in cardiomyocytes.Molecular pharmacology · 2009Article
- Meiotic resumption in response to luteinizing hormone is independent of a Gi family G protein or calcium in the mouse oocyte.Developmental biology · 2006Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
1. Profiles of G protein activation have been assessed using a [35S]-GTPgammaS binding/immunoprecipitation strategy in Chinese hamster ovary cells expressing either M1, M2, M3 or M4 muscarinic acetylcholine (mACh) receptor subtypes, where expression levels of M1 and M3, or M2 and M4 receptors were approximately equal. 2. Maximal [35S]-GTPgammaS binding to G(q/11)alpha stimulated by M1/M3 receptors, or G(i1-3)alpha stimulated by M2/M4 receptors occurred within approximately 2 min of agonist addition. The increases in G(q/11)alpha-[35S]-GTPgammaS binding after M1 and M3 receptor stimulation differed substantially, with M1 receptors causing a 2-3 fold greater increase in [35S]-GTPgammaS binding and requiring 5 fold lower concentrations of methacholine to stimulate a half-maximal response. 3. Comparison of M2 and M4 receptor-mediated G(i1-3)alpha-[35S]-GTPgammaS binding also revealed differences, with M2 receptors causing a greater increase in G(i1-3)alpha activation and requiring 10 fold lower concentrations of methacholine to stimulate a half-maximal response. 4. Comparison of methacholine- and pilocarpine-mediated effects revealed that the latter partial agonist is more effective in activating G(i3)alpha compared to G(i1/2)alpha for both M2 and M4 receptors. More marked agonist/partial agonist differences were observed with respect to M1/M3-mediated stimulations of G(q/11)alpha- and G(i1-3)alpha-[35S]-GTPgammaS binding. Whereas coupling to these Galpha subclasses decreased proportionately for M1 receptor stimulation by these agonists, pilocarpine possesses a greater intrinsic activity at M3 receptors for G(i)alpha versus G(q/11)alpha activation. 5. These data demonstrate that mACh receptor subtype and the nature of the agonist used govern the repertoire of G proteins activated. They also provide insights into how the diversity of coupling can be pharmacologically exploited, and provide a basis for a better understanding of how multiple receptor subtypes can be differentially regulated.
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