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GPR75 Receptor Antibodies

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Immunohistochemical identification of Threonine 427/Serine429 phosphorylation of G-protein coupled Receptor 75 in mouse brain.
pT427/pS429-GPR75 (IHC grade phospho-GPR75...
Threonine427/Serine429 (T427/S429) is a major phosphorylation site of the human GPR75 receptor. The pT427/pS429-GPR75 antibody detects GRK-mediated constitutive phosphorylation of GPR75 when expressed in HEK293 cells.
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The endogenous ligand for GPR75 is still unknown. The chemokine CCL5/RANTES was reported to be an agonist of GPR75 but the pairing could not be repeated in β-arrestin assays. It has been reported that people with protein-truncating variants of GPR75 were associated with 5.3 kg lower body weight and 54% lower odds for obesity. GPR75 knock-out mice showed resistance to weight gain under high-fat diet. GPR75 is constitutively phosphorylated by GRKs when expressed in HEK293 cells at carboxyl-terminal serine422/serine423 (pS422/pS423-GPR75) and threonine427/serine429 (pT427/pS429-GPR75). Serine422/serine423 is also substrate for PKC-mediated phosphorylation. This nomenclature refers to the human GPR75 receptor. This phosphorylation motif is highly conserved across species and is identical mice, rats and humans. For more information on GPR75 pharmacology please refer to the IUPHAR database. For further reading refer to:

Akbari P, Gilani A, Sosina O, Kosmicki JA, Khrimian L, Fang YY, Persaud T, Garcia V, Sun D, Li A, Mbatchou J, Locke AE, Benner C, Verweij N, Lin N, Hossain S, Agostinucci K, Pascale JV, Dirice E, Dunn M; Regeneron Genetics Center; DiscovEHR Collaboration; Kraus WE, Shah SH et al. Sequencing of 640,000 exomes identifies GPR75 variants associated with protection from obesity. Science. 2021 Jul 2;373(6550):eabf8683. doi: 10.1126/science.abf8683. PMID: 34210852; PMCID: PMC10275396.

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 endogenous ligand for GPR75 is still unknown. The chemokine CCL5/RANTES was reported to be an agonist of GPR75 but the pairing could not be repeated in β-arrestin assays. It has been... read more »
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GPR75 Receptor Antibodies

The endogenous ligand for GPR75 is still unknown. The chemokine CCL5/RANTES was reported to be an agonist of GPR75 but the pairing could not be repeated in β-arrestin assays. It has been reported that people with protein-truncating variants of GPR75 were associated with 5.3 kg lower body weight and 54% lower odds for obesity. GPR75 knock-out mice showed resistance to weight gain under high-fat diet. GPR75 is constitutively phosphorylated by GRKs when expressed in HEK293 cells at carboxyl-terminal serine422/serine423 (pS422/pS423-GPR75) and threonine427/serine429 (pT427/pS429-GPR75). Serine422/serine423 is also substrate for PKC-mediated phosphorylation. This nomenclature refers to the human GPR75 receptor. This phosphorylation motif is highly conserved across species and is identical mice, rats and humans. For more information on GPR75 pharmacology please refer to the IUPHAR database. For further reading refer to:

Akbari P, Gilani A, Sosina O, Kosmicki JA, Khrimian L, Fang YY, Persaud T, Garcia V, Sun D, Li A, Mbatchou J, Locke AE, Benner C, Verweij N, Lin N, Hossain S, Agostinucci K, Pascale JV, Dirice E, Dunn M; Regeneron Genetics Center; DiscovEHR Collaboration; Kraus WE, Shah SH et al. Sequencing of 640,000 exomes identifies GPR75 variants associated with protection from obesity. Science. 2021 Jul 2;373(6550):eabf8683. doi: 10.1126/science.abf8683. PMID: 34210852; PMCID: PMC10275396.

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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