ArticleThe Journal of biological chemistry2009
The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1.
Article in The Journal of biological chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers.
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Who cites it
37 citing papers in PubMed, 76 citations in OpenAlex.
- Thiazolidinediones (TZDs) enhance insulin secretory response via GPR40 and adenylate cyclase (AC).Journal of cellular physiology · 2021Article
- The N-terminus of GPR37L1 is proteolytically processed by matrix metalloproteases.Scientific reports · 2020Article
- Obesity-induced asthma: Role of free fatty acid receptors.The Japanese dental science review · 2019Review
- Upregulation of free fatty acid receptors in periodontal tissues of patients with metabolic syndrome and periodontitis.Journal of periodontal research · 2019Article
- FFAR4 Is Involved in Regulation of Neurotensin Release From Neuroendocrine Cells and Male C57BL/6 Mice.Endocrinology · 2018Article
- The free fatty acid receptor 1 promotes airway smooth muscle cell proliferation through MEK/ERK and PI3K/Akt signaling pathways.American journal of physiology. Lung cellular and molecular physiology · 2018Article
- SAR Studies of Indole-5-propanoic Acid Derivatives To Develop Novel GPR40 Agonists.ACS medicinal chemistry letters · 2017Article
- PPARγ signaling and emerging opportunities for improved therapeutics.Pharmacological research · 2016Review
- G Protein-coupled Receptor 40 (GPR40) and Peroxisome Proliferator-activated Receptor γ (PPARγ): AN INTEGRATED TWO-RECEPTOR SIGNALING PATHWAY.The Journal of biological chemistry · 2015Article
- Characterizing pharmacological ligands to study the long-chain fatty acid receptors GPR40/FFA1 and GPR120/FFA4.British journal of pharmacology · 2015Review
- A Single Amino Acid Mutation (R104P) in the E/DRY Motif of GPR40 Impairs Receptor Function.PloS one · 2015Article
- Breaking the mold: transcription factors in the anucleate platelet and platelet-derived microparticles.Frontiers in immunology · 2015Review
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.Molecular pharmacology · 2013Article
- Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids.Molecular endocrinology (Baltimore, Md.) · 2013Review
- The free fatty acid receptor G protein-coupled receptor 40 (GPR40) protects from bone loss through inhibition of osteoclast differentiation.The Journal of biological chemistry · 2013Article
- Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2012Article
- Identification and pharmacological characterization of multiple allosteric binding sites on the free fatty acid 1 receptor.Molecular pharmacology · 2012Article
- G protein-coupled receptors for energy metabolites as new therapeutic targets.Nature reviews. Drug discovery · 2012Review
- Thiazolidinediones induce osteocyte apoptosis by a G protein-coupled receptor 40-dependent mechanism.The Journal of biological chemistry · 2012Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
The endogenous ligands for free fatty acid receptor 1 (FFA1) are medium and longer chain free fatty acids. However, a range of selective, small molecule ligands have recently been developed as tool compounds to explore the therapeutic potential of this receptor, whereas clinically employed thiazolidinedione "glitazone" drugs are also agonists at FFA1. Each of these classes of agonist was able to promote phosphorylation of the ERK1/2 mitogen-activated protein (MAP) kinases in cells able to express human FFA1 on demand. However, although both lauric acid and the synthetic agonist GW9508X produced rapid and transient ERK1/2 MAP kinase phosphorylation, the thiazolidinedione rosiglitazone produced responses that were sustained for a substantially longer period. Despite this difference, the effects of each ligand required FFA1 and were transduced in each case predominantly via G proteins of the Galphaq/Galpha11 family. Different glitazone drugs also displayed markedly different efficacy and kinetics of sustainability of ERK1/2 MAP kinase phosphorylation. A number of orthosteric binding site mutants of FFA1 were generated, and despite variations in the changes of potency and efficacy of the three ligand classes in different functional end point assays, these were consistent with rosiglitazone also binding at the orthosteric site. Four distinct polymorphic variants of human FFA1 have been described. Despite previous indications that these display differences in function and pharmacology, they all responded in entirely equivalent ways to lauric acid, rosiglitazone, and GW9508X in measures of ERK1/2 MAP kinase phosphorylation, enhancement of binding of [35S]GTPgammaS (guanosine 5'-O-(3-[35S]thio)triphosphate) to Galphaq, and elevation of intracellular [Ca2+], suggesting that individuals expressing each variant are likely to respond equivalently to orthosteric agonists of FFA1.
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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.