ArticleBritish journal of pharmacology2014
Investigating G protein signalling bias at the glucagon-like peptide-1 receptor in yeast.
Article in British journal of pharmacology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 54 citations in OpenAlex.
- Effects of Membrane Cholesterol on the Structure and Function of Selected Class A GPCRs─Challenges and Future Perspectives.Biochemistry · 2025Review
- Receptor activity-modifying protein 3 enhances GLP-1-mediated insulin secretion.The Journal of biological chemistry · 2025Article
- Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.Journal of cell science · 2025Review
- Exploring GPCR conformational dynamics using single-molecule fluorescence.Methods (San Diego, Calif.) · 2024Review
- Engineered cell differentiation and sexual reproduction in probiotic and mating yeasts.Nature communications · 2022Article
- Signaling pathways in obesity: mechanisms and therapeutic interventions.Signal transduction and targeted therapy · 2022Review
- Functional expression of opioid receptors and other human GPCRs in yeast engineered to produce human sterols.Nature communications · 2022Article
- The therapeutic potential of GLP-1 receptor biased agonism.British journal of pharmacology · 2022 · on this mapReview
- Activation of glucagon-like peptide-1 receptors and skilled reach foraging.Addiction biology · 2021Article
- Structure-based identification of dual ligands at the AJournal of cheminformatics · 2021Article
- Metabolic Functions of G Protein-Coupled Receptors and β-Arrestin-Mediated Signaling Pathways in the Pathophysiology of Type 2 Diabetes and Obesity.Frontiers in endocrinology · 2021Review
- Gs/Gq signaling switch in β cells defines incretin effectiveness in diabetes.The Journal of clinical investigation · 2020Article
- Glucagon-like peptide-1 receptor regulation of basal dopamine transporter activity is species-dependent.Neurochemistry international · 2020Article
- Receptor component protein, an endogenous allosteric modulator of family B G protein coupled receptors.Biochimica et biophysica acta. Biomembranes · 2020Article
- Expression and purification of recombinant G protein-coupled receptors: A review.Protein expression and purification · 2020Review
- Article
- Hepatic Glucagon Receptor Signaling Enhances Insulin-Stimulated Glucose Disposal in Rodents.Diabetes · 2018Article
- Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.The Journal of biological chemistry · 2018Article
- Loss of dorsomedial hypothalamic GLP-1 signaling reduces BAT thermogenesis and increases adiposity.Molecular metabolism · 2018 · on this mapArticle
- Proinflammatory switch from Gαs to Gαi signaling by Glucagon-like peptide-1 receptor in murine splenic monocyte following burn injury.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2018Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
background and purposeThe glucagon-like peptide 1 (GLP-1) receptor performs an important role in glycaemic control, stimulating the release of insulin. It is an attractive target for treating type 2 diabetes. Recently, several reports of adverse side effects following prolonged use of GLP-1 receptor therapies have emerged: most likely due to an incomplete understanding of signalling complexities. EXPERIMENTAL APPROACH: We describe the expression of the GLP-1 receptor in a panel of modified yeast strains that couple receptor activation to cell growth via single Gα/yeast chimeras. This assay enables the study of individual ligand-receptor G protein coupling preferences and the quantification of the effect of GLP-1 receptor ligands on G protein selectivity. KEY
resultsThe GLP-1 receptor functionally coupled to the chimeras representing the human Gαs, Gαi and Gαq subunits. Calculation of the dissociation constant for a receptor antagonist, exendin-3 revealed no significant difference between the two systems. We obtained previously unobserved differences in G protein signalling bias for clinically relevant therapeutic agents, liraglutide and exenatide; the latter displaying significant bias for the Gαi pathway. We extended the use of the system to investigate small-molecule allosteric compounds and the closely related glucagon receptor. CONCLUSIONS AND IMPLICATIONS: These results provide a better understanding of the molecular events involved in GLP-1 receptor pleiotropic signalling and establish the yeast platform as a robust tool to screen for more selective, efficacious compounds acting at this important class of receptors in the future.
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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.