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GPR119 Receptor Antibodies

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Validation of the GPR119 Receptor in transfected HEK293 cells
GPR119 (non-phospho), G protein-coupled...
The non-phospho-GPR119 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR119. It can be used to detect total GPR119 receptors in Western blots independent of phosphorylation. The GPR119...
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The G protein–coupled receptor 119 (GPR119) is a class A GPCR primarily coupled to the Gs protein, leading to activation of adenylyl cyclase, increased intracellular cAMP, and subsequent enhancement of hormone and insulin secretion. GPR119 is expressed predominantly in pancreatic β-cells and enteroendocrine cells of the small intestine, particularly L and K cells, which release glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), respectively. Endogenous ligands for GPR119 include oleoylethanolamide (OEA) and related lipid-derived metabolites, while numerous synthetic agonists have been developed for potential treatment of type 2 diabetes mellitus and obesity. Functionally, GPR119 activation enhances glucose-dependent insulin secretion from β-cells and incretin hormone release from intestinal cells, thereby improving glucose tolerance without causing hypoglycemia. The receptor’s restricted expression pattern and glucose-dependent mechanism make it an attractive therapeutic target with a favorable safety profile compared to direct insulin secretagogues. However, clinical outcomes with synthetic GPR119 agonists have been modest, likely due to limited receptor reserve or compensatory metabolic pathways. Beyond metabolism, GPR119 may also play roles in lipid sensing and energy homeostasis in the gut–pancreas axis. Overall, GPR119 acts as a nutrient-sensing receptor that links dietary lipid metabolism to incretin and insulin release, offering valuable but as yet unrealized potential for metabolic disease therapy. For more information on GPR119 pharmacology please refer to the IUPHAR database. For further reading refer to:

Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR, Pin JP, Spedding M, Harmar AJ. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev. 2013 May 17;65(3):967-86. doi: 10.1124/pr.112.007179. PMID: 23686350; PMCID: PMC3698937.

Alexander SP, Battey J, Benson HE, Benya RV, Bonner TI, Davenport AP, Dhanachandra Singh K, Eguchi S, Harmar A, Holliday N, Jensen RT, Karnik S, Kostenis E, Liew WC, Monaghan AE, Mpamhanga C, Neubig R, Pawson AJ, Pin JP, Sharman JL, Spedding M, Spindel E, Stoddart L, Storjohann L, Thomas WG, Tirupula K, Vanderheyden P. Class A Orphans in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F16/2023.1.

The G protein–coupled receptor 119 (GPR119) is a class A GPCR primarily coupled to the Gs protein, leading to activation of adenylyl cyclase, increased intracellular cAMP, and subsequent... read more »
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GPR119 Receptor Antibodies

The G protein–coupled receptor 119 (GPR119) is a class A GPCR primarily coupled to the Gs protein, leading to activation of adenylyl cyclase, increased intracellular cAMP, and subsequent enhancement of hormone and insulin secretion. GPR119 is expressed predominantly in pancreatic β-cells and enteroendocrine cells of the small intestine, particularly L and K cells, which release glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), respectively. Endogenous ligands for GPR119 include oleoylethanolamide (OEA) and related lipid-derived metabolites, while numerous synthetic agonists have been developed for potential treatment of type 2 diabetes mellitus and obesity. Functionally, GPR119 activation enhances glucose-dependent insulin secretion from β-cells and incretin hormone release from intestinal cells, thereby improving glucose tolerance without causing hypoglycemia. The receptor’s restricted expression pattern and glucose-dependent mechanism make it an attractive therapeutic target with a favorable safety profile compared to direct insulin secretagogues. However, clinical outcomes with synthetic GPR119 agonists have been modest, likely due to limited receptor reserve or compensatory metabolic pathways. Beyond metabolism, GPR119 may also play roles in lipid sensing and energy homeostasis in the gut–pancreas axis. Overall, GPR119 acts as a nutrient-sensing receptor that links dietary lipid metabolism to incretin and insulin release, offering valuable but as yet unrealized potential for metabolic disease therapy. For more information on GPR119 pharmacology please refer to the IUPHAR database. For further reading refer to:

Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR, Pin JP, Spedding M, Harmar AJ. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev. 2013 May 17;65(3):967-86. doi: 10.1124/pr.112.007179. PMID: 23686350; PMCID: PMC3698937.

Alexander SP, Battey J, Benson HE, Benya RV, Bonner TI, Davenport AP, Dhanachandra Singh K, Eguchi S, Harmar A, Holliday N, Jensen RT, Karnik S, Kostenis E, Liew WC, Monaghan AE, Mpamhanga C, Neubig R, Pawson AJ, Pin JP, Sharman JL, Spedding M, Spindel E, Stoddart L, Storjohann L, Thomas WG, Tirupula K, Vanderheyden P. Class A Orphans in GtoPdb v.2023.1. IUPHAR/BPS Guide to Pharmacology CITE. 2023; 2023(1). Available from: https://doi.org/10.2218/gtopdb/F16/2023.1.

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