ArticlePloS one2017
The acute glucose lowering effect of specific GPR120 activation in mice is mainly driven by glucagon-like peptide 1.
Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 51 citations in OpenAlex.
- Free fatty acid receptor 4 agonism stimulates insulin secretion via different mechanisms in mouse vs human islets.Endocrinology · 2026Article
- Sphinganine as a novel stimulator of GLP-1 secretion.Diabetologia · 2026Article
- Mediterranean Diet Can Reduce Fat Accumulation and Obesity Progression Through Action of Plant Bioactive Molecules.International journal of molecular sciences · 2026Review
- The Multifaceted Roles of GPR120 in Central Nervous System Disorders: Mechanistic Insights and Therapeutic Implications.Molecular neurobiology · 2026Review
- Potential Therapeutic Exploitation of G Protein-Coupled Receptor 120 (GPR120/FFAR4) Signaling in Obesity-Related Metabolic Disorders.International journal of molecular sciences · 2025Review
- Biased agonism at free-fatty acid receptor-4 (FFA4/GPR120).Pharmacology & therapeutics · 2025Review
- Novel Phenoxyalkanoic Acid Derivatives as Free Fatty Acid Receptor 4 Agonists for Treating Type 2 Diabetes Mellitus.International journal of molecular sciences · 2024Article
- Cellular mechanisms of incretin hormone secretion.Journal of molecular endocrinology · 2024Review
- Single-cell transcriptomic atlas of enteroendocrine cells along the murine gastrointestinal tract.PloS one · 2024Article
- Role of EP4 factor in paediatric type 1 diabetes mellitus: a comprehensive review focusing on the honeymoon period.Pediatric endocrinology, diabetes, and metabolism · 2024Review
- The Effects of Artificial Sweeteners on Intestinal Nutrient-Sensing Receptors: Dr. Jekyll or Mr. Hyde?Life (Basel, Switzerland) · 2023Review
- Endocrine, genetic, and microbiome nexus of obesity and potential role of postbiotics: a narrative review.Eating and weight disorders : EWD · 2023Review
- Optimization of First-in-Class Dual-Acting FFAR1/FFAR4 Allosteric Modulators with Novel Mode of Action.ACS medicinal chemistry letters · 2022Article
- Comment on "Activation of the Omega-3 Fatty Acid Receptor GPR120 Protects against Focal Cerebral Ischemic Injury by Preventing Inflammation and Apoptosis in Mice".Journal of immunology (Baltimore, Md. : 1950) · 2022Article
- Revisiting the concept of incretin and enteroendocrine L-cells as type 2 diabetes mellitus treatment.Pharmacological research · 2022Review
- Involvement of Gut Microbial Metabolites Derived from Diet on Host Energy Homeostasis.International journal of molecular sciences · 2022Review
- The Impact of Diet on Bone and Fracture Risk in Diabetes.Current osteoporosis reports · 2022Review
- Free fatty acid receptors in the endocrine regulation of glucose metabolism: Insight from gastrointestinal-pancreatic-adipose interactions.Frontiers in endocrinology · 2022Review
- Discovery of ciliary G protein-coupled receptors regulating pancreatic islet insulin and glucagon secretion.Genes & development · 2021Article
- GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery.Journal of medicinal chemistry · 2021Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The mechanism behind the glucose lowering effect occurring after specific activation of GPR120 is not completely understood. In this study, a potent and selective GPR120 agonist was developed and its pharmacological properties were compared with the previously described GPR120 agonist Metabolex-36. Effects of both compounds on signaling pathways and GLP-1 secretion were investigated in vitro. The acute glucose lowering effect was studied in lean wild-type and GPR120 null mice following oral or intravenous glucose tolerance tests. In vitro, in GPR120 overexpressing cells, both agonists signaled through Gαq, Gαs and the β-arrestin pathway. However, in mouse islets the signaling pathway was different since the agonists reduced cAMP production. The GPR120 agonists stimulated GLP-1 secretion both in vitro in STC-1 cells and in vivo following oral administration. In vivo GPR120 activation induced significant glucose lowering and increased insulin secretion after intravenous glucose administration in lean mice, while the agonists had no effect in GPR120 null mice. Exendin 9-39, a GLP-1 receptor antagonist, abolished the GPR120 induced effects on glucose and insulin following an intravenous glucose challenge. In conclusion, GLP-1 secretion is an important mechanism behind the acute glucose lowering effect following specific GPR120 activation.
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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.