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GPR146 Receptor Antibodies

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Validation of the GPR146 Receptor in transfected HEK293 cells
GPR146 (non-phospho), G protein-coupled...
The non-phospho-GPR146 receptor antibody is directed against the distal end of the carboxyl-terminal tail of human GPR146. It can be used to detect total GPR146 receptors in Western blots independent of phosphorylation. The GPR146...
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The G protein–coupled receptor 146 (GPR146) is an orphan class A GPCR whose endogenous ligand and detailed signaling mechanisms remain incompletely defined. Pharmacologically, studies suggest that GPR146 may couple to Gs proteins, leading to cAMP accumulation, although definitive characterization of its ligand and downstream effectors is still under investigation. GPR146 is broadly expressed in metabolically active tissues, including the liver, adipose tissue, and endothelial cells, as well as in immune and hematopoietic lineages at lower levels. Genetic and functional studies have identified GPR146 as an important regulator of lipid metabolism and cholesterol homeostasis: Gpr146 knockout mice show reduced plasma cholesterol and protection against atherosclerosis, likely due to altered hepatic gene expression and lipid processing. Human genome-wide association studies (GWAS) have linked GPR146 variants to serum cholesterol and LDL-C levels, underscoring its relevance in cardiometabolic disease. Although the receptor’s endogenous ligand is still unknown, some data suggest that serum-derived or lipid-related molecules may activate GPR146, indicating a role in nutrient or metabolic sensing. Functionally, GPR146 may modulate hepatic lipoprotein production, vascular signaling, and systemic lipid homeostasis. Overall, GPR146 is emerging as a novel metabolic GPCR with potential as a therapeutic target for dyslipidemia and cardiovascular disease, pending further elucidation of its signaling pathways and physiological ligands. For more information on GPR146 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 146 (GPR146) is an orphan class A GPCR whose endogenous ligand and detailed signaling mechanisms remain incompletely defined. Pharmacologically, studies suggest that... read more »
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GPR146 Receptor Antibodies

The G protein–coupled receptor 146 (GPR146) is an orphan class A GPCR whose endogenous ligand and detailed signaling mechanisms remain incompletely defined. Pharmacologically, studies suggest that GPR146 may couple to Gs proteins, leading to cAMP accumulation, although definitive characterization of its ligand and downstream effectors is still under investigation. GPR146 is broadly expressed in metabolically active tissues, including the liver, adipose tissue, and endothelial cells, as well as in immune and hematopoietic lineages at lower levels. Genetic and functional studies have identified GPR146 as an important regulator of lipid metabolism and cholesterol homeostasis: Gpr146 knockout mice show reduced plasma cholesterol and protection against atherosclerosis, likely due to altered hepatic gene expression and lipid processing. Human genome-wide association studies (GWAS) have linked GPR146 variants to serum cholesterol and LDL-C levels, underscoring its relevance in cardiometabolic disease. Although the receptor’s endogenous ligand is still unknown, some data suggest that serum-derived or lipid-related molecules may activate GPR146, indicating a role in nutrient or metabolic sensing. Functionally, GPR146 may modulate hepatic lipoprotein production, vascular signaling, and systemic lipid homeostasis. Overall, GPR146 is emerging as a novel metabolic GPCR with potential as a therapeutic target for dyslipidemia and cardiovascular disease, pending further elucidation of its signaling pathways and physiological ligands. For more information on GPR146 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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