ArticleProceedings of the National Academy of Sciences of the United States of America2023
Molecular mechanism of fatty acid activation of FFAR1.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 33 citations in OpenAlex.
- GPR40 Attenuates Glioma TMZ-Resistance Through Ferroptosis Inhibition.Neurochemical research · 2026Article
- Insulin Resistance and Inflammation.International journal of molecular sciences · 2026Review
- GPCR-Mediated Cell Intelligence: A Potential Mechanism for Survival and Long-Term Health.Current issues in molecular biology · 2026Review
- Strategic advances for cryo-EM structural studies of small (<100 kDa) GPCRs.Communications biology · 2026Review
- Long-chain fatty acids as functional modulators in PCOS: metabolic crosstalk, signaling pathways, and therapeutic implications.Frontiers in nutrition · 2026Review
- Effect of a Low Electrostatic Environment on the Helical Structures of Peptides and Proteins Using Flexible Water Models: An In Silico Study.ACS omega · 2025Article
- Bitopic AJournal of medicinal chemistry · 2025Article
- Multicolored sequential resonance energy transfer for detection of simultaneous ligand binding at G protein-coupled receptors.Nature communications · 2025Article
- G-protein coupled receptors in metabolic reprogramming and cancer.Pharmacology & therapeutics · 2025Review
- Structural insights into lipid chain-length selectivity and allosteric regulation of FFA2.Nature communications · 2025Article
- A non-canonical mechanism of GPCR activation.Nature communications · 2024Article
- Structural mechanisms of potent lysophosphatidic acid receptor 1 activation by nonlipid basic agonists.Communications biology · 2024Article
- GPR40/GPR120 Agonist GW9508 Improves Metabolic Syndrome-Exacerbated Periodontitis in Mice.International journal of molecular sciences · 2024Article
- Influence of the Water Model on the Structure and Interactions of the GPR40 Protein with the Lipid Membrane and the Solvent: Rigid versus Flexible Water Models.Journal of chemical theory and computation · 2024Article
- Beneath the surface: endosomal GPCR signaling.Trends in biochemical sciences · 2024Review
- Cryo-EM structure of cell-free synthesized human histamine 2 receptor/GNature communications · 2024Article
- Structural basis for the ligand recognition and signaling of free fatty acid receptors.Science advances · 2024Article
- Structural insights into an intracellular biased agonist for GPCRs.Nature structural & molecular biology · 2023Article
- How important are fatty acids in human health and can they be used in treating diseases?Gut microbesReview
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
FFAR1 is a G-protein-coupled receptor (GPCR) that responds to circulating free fatty acids to enhance glucose-stimulated insulin secretion and release of incretin hormones. Due to the glucose-lowering effect of FFAR1 activation, potent agonists for this receptor have been developed for the treatment of diabetes. Previous structural and biochemical studies of FFAR1 showed multiple sites of ligand binding to the inactive state but left the mechanism of fatty acid interaction and receptor activation unknown. We used cryo-electron microscopy to elucidate structures of activated FFAR1 bound to a G
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Registered trials
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.