ArticleBritish journal of pharmacology2004
Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist-specific G protein activation.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers, 1 of them a synthesis that pooled it.
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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
41 citing papers in PubMed, 1 synthesis or guideline pooled it, 79 citations in OpenAlex.
- Purinergic system dysfunction in mood disorders: a key target for developing improved therapeutics.Progress in neuro-psychopharmacology & biological psychiatry · 2015Pooled it
- Adenosine Receptor Functionality and Desensitization Machinery in a Neuronal Cell Model of Angelman Syndrome.Journal of developmental biology · 2026Article
- Photoswitchable Diazocine Derivative for Adenosine AJournal of the American Chemical Society · 2025Article
- Extracellular purines in lung endothelial permeability and pulmonary diseases.Frontiers in physiology · 2024Review
- New paradigms in purinergic receptor ligand discovery.Neuropharmacology · 2023Review
- Selective activation of Gαob by an adenosine ANature communications · 2022Article
- Molecular Simulations and Drug Discovery of Adenosine Receptors.Molecules (Basel, Switzerland) · 2022Review
- G protein-coupled receptor-effector macromolecular membrane assemblies (GEMMAs).Pharmacology & therapeutics · 2022Review
- The Impact of the Secondary Binding Pocket on the Pharmacology of Class A GPCRs.Frontiers in pharmacology · 2022Review
- Optimization of the Heterologous Expression of the Cannabinoid Type-1 (CBFrontiers in endocrinology · 2021Article
- The Signaling Pathways Involved in the Anticonvulsive Effects of the Adenosine AInternational journal of molecular sciences · 2020Review
- Allosteric modulation of adenosine A1 and cannabinoid 1 receptor signaling by G-peptides.Pharmacology research & perspectives · 2020Article
- NanoBiT Complementation to Monitor Agonist-Induced Adenosine ASLAS discovery : advancing life sciences R & D · 2020Article
- Mechanistic Insights into Specific G Protein Interactions with Adenosine Receptors.The journal of physical chemistry. B · 2019Article
- Calcium receptor signaling and citrate transport.Urolithiasis · 2018Article
- Increased Gi protein signaling potentiates the negative chronotropic effect of adenosine in the SHR right atrium.Naunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Modelling and simulation of biased agonism dynamics at a G protein-coupled receptor.Journal of theoretical biology · 2018Article
- AMolecular neurobiology · 2017Review
- Purinergic Receptor Expression and Potential Association with Human Embryonic Stem Cell-Derived Oligodendrocyte Progenitor Cell Development.Cell journal · 2017Article
- On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin.Biochemical pharmacology · 2016Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The present study investigates the effect of varying ligand structure on the ability of agonists to activate guanine nucleotide-binding proteins of the Gi, Gs and Gq families via the A(1) adenosine receptor. In CHO cells expressing this receptor, inhibition or potentiation of forskolin-stimulated cAMP accumulation was used as an end point to measure the activation of Gi and, in Pertussis toxin (PTX)-treated cells, Gs, respectively. Stimulation of inositol phosphate accumulation in PTX-treated cells was used as an index of Gq activation. CPA (N(6)-cyclopentyladenosine), NECA (5'-N-ethyl-carboxyamidoadenosine) and eight analogues of these ligands presented a range of guanine nucleotide-binding protein (G-protein)-activating profiles. Some ligands could only activate Gi (e.g. 2'deoxyCPA), some primarily Gi and Gs (and only weakly Gq) (e.g. 3'deoxyCPA), highlighting the importance of the ribose hydroxyls in agonist activation of multiple G proteins. CHA (N(6)-cyclohexyladenosine) activated Gi, Gs and Gq, but was more efficacious than CPA in activating Gs. The NECA analogues 5'-N-cyclopropyl-carboxamidoadenosine, 5'-N-cyclobutyl-carboxamidoadenosine and 5'-N-cyclopentyl-carboxamidoadenosine (CPeCA) also activated all three G proteins, although their ability to activate Gs and Gq (relative to CPA) was reduced with increasing substituent size, such that CPeCA produced only a small stimulation (at 100 microM) at Gq, but was a full agonist, relative to CPA, at Gi and Gs. This study suggests that the A(1) adenosine receptor can adopt agonist-specific conformations, arising from small changes in ligand structure, which lead to the differential activation of Gi, Gs and Gq.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.