Target intelligence / Profile preview

G protein-coupled receptor 83 (GPR83)

Target
GPR83
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

G protein-coupled receptor 83 (GPR83) is an orphan GPCR, predominantly expressed in the brain (notably the hypothalamic arcuate nucleus) and thymus, functioning primarily in neuropeptide signaling, energy metabolism, and body weight regulation. Identified ligands include the neuropeptide PEN, and mouse model studies indicate that loss of GPR83 protects against diet-induced obesity, underscoring its role in metabolic control. GPR83 can form both homodimers and heterodimers (notably with the ghrelin receptor), potentially modulating activity of other GPCRs. Endogenous activation and detailed signaling mechanisms remain an area of active research, with the receptor implicated in Gq/11 and Gi protein-mediated pathways and basal MAPK activation. There is currently no established targeted therapeutic drug, but its function and expression pattern suggest relevance for metabolic disorders, obesity, and some CNS diseases.

Other names
GPR72JP05G-protein coupled receptor 72GIRglucocorticoid-induced receptorprobable G protein-coupled receptor 83
02

Mechanism of action

Modulates intracellular signaling via Gq/11 and Gi protein pathways; Involved in regulation of basal and ligand-dependent signaling; PEN-induced effects via G proteins

03

Biological functions

Signal transductionNeuropeptide signalingRegulation of energy metabolismFood intake and body weight regulationRegulation of anxiety-related behaviors
04

Disease associations

ObesityThalamic diseasePotential involvement in Alzheimer's disease and other neurological disorders
05

Safety considerations

no reported safety-specific concerns, but modulation may influence metabolic and possibly neuroendocrine functions
06

Interacting drugs

None established as approved therapeutic drugs. The neuropeptide PEN is identified as an endogenous ligand.
07

Biomarkers

no documented clinical biomarkers for patient selection or efficacy monitoring specific to GPR83

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