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GPR4 Receptor Antibodies

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GPR4 (non-phospho), G protein-coupled Receptor 4 Antibody
GPR4 (non-phospho), G protein-coupled Receptor...
The non-phospho-GPR4 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR4. It can be used to detect total GPR4 receptors in Western blots independent of phosphorylation. The GPR4 antibody can...
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G protein-coupled receptor 4 (GPR4), encoded by GPR4, is a class A receptor activated by extracellular acidification. Protonation of extracellular amino acid residues alters receptor conformation, allowing GPR4 to detect pH changes around the physiological range. It couples prominently to Gs, stimulating adenylyl cyclase and increasing intracellular cAMP, but can also engage Gq/11 and G12/13 pathways. GPR4 is highly expressed in vascular endothelial cells and is also found in the kidney and selected brainstem neurons. In endothelial cells, acid-induced GPR4 activation can increase adhesion molecule and chemokine expression, promoting leukocyte recruitment. Animal studies also implicate GPR4 in renal acid–base regulation and respiratory responses to carbon dioxide. Its activation is strongly dependent on extracellular pH, while the mechanisms governing phosphorylation, desensitization, and trafficking remain incompletely characterized. The orally bioavailable antagonist NE52-QQ57 is used in preclinical studies of GPR4 function. No GPR4-selective drug has been reported to enter clinical trials or receive approval for therapeutic use. For more information on GPR4 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.

G protein-coupled receptor 4 (GPR4), encoded by GPR4 , is a class A receptor activated by extracellular acidification. Protonation of extracellular amino acid residues alters receptor... read more »
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GPR4 Receptor Antibodies

G protein-coupled receptor 4 (GPR4), encoded by GPR4, is a class A receptor activated by extracellular acidification. Protonation of extracellular amino acid residues alters receptor conformation, allowing GPR4 to detect pH changes around the physiological range. It couples prominently to Gs, stimulating adenylyl cyclase and increasing intracellular cAMP, but can also engage Gq/11 and G12/13 pathways. GPR4 is highly expressed in vascular endothelial cells and is also found in the kidney and selected brainstem neurons. In endothelial cells, acid-induced GPR4 activation can increase adhesion molecule and chemokine expression, promoting leukocyte recruitment. Animal studies also implicate GPR4 in renal acid–base regulation and respiratory responses to carbon dioxide. Its activation is strongly dependent on extracellular pH, while the mechanisms governing phosphorylation, desensitization, and trafficking remain incompletely characterized. The orally bioavailable antagonist NE52-QQ57 is used in preclinical studies of GPR4 function. No GPR4-selective drug has been reported to enter clinical trials or receive approval for therapeutic use. For more information on GPR4 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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