Target intelligence / Profile preview

G protein-coupled receptor 82 (GPR82)

Target
GPR82
Molecular classification
G protein-coupled receptor, Receptor, Rhodopsin-like class A GPCR
01

Overview

G protein-coupled receptor 82 (GPR82) is an orphan G protein-coupled receptor of the rhodopsin-like class A family, containing seven transmembrane domains and localized to the cell membrane[2][4]. Its endogenous ligand and precise physiological function remain unknown, though evidence from genetic and animal studies suggests involvement in energy balance, lipid metabolism, and metabolic syndrome phenotypes. GPR82 has been shown to modulate food intake, body weight, serum triacylglyceride levels, insulin sensitivity, and glucose tolerance in mouse models, especially under conditions mimicking Western diets. Structure–function analyses and phylogeny predict possible lipid-based ligand interactions, notably with N-arachidonylglycine, indicating a candidate role in lipid signaling pathways. Despite gene-disease association studies linking GPR82 to metabolic diseases, it has not yet been validated as a clinical drug target, and no approved drugs act on it directly[1][3][4].

Other names
Probable G-protein coupled receptor 82Putative G-protein coupled receptor 82GPR82
02

Mechanism of action

Not established. No approved or widely-studied drugs are documented to target GPR82 directly. Functional mouse studies suggest modulation of receptor activity impacts metabolic parameters, but pharmacological mechanisms remain undefined[1][3].

03

Biological functions

Signal transductionLipid signaling (inferred from possible ligand association with N-arachidonylglycine[1])Regulation of energy balance[1]
04

Disease associations

Metabolic syndromeAbdominal obesityInsulin resistance[1][3]
05

Safety considerations

As a putative metabolic regulator, potential impacts on glucose homeostasis, lipid metabolism, and cardiovascular function could be relevant, but no specific therapeutic safety data exist due to the lack of clinical targeting[1].

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