Target intelligence / Profile preview

G protein-coupled receptor 37 (GPR37)

Target
GPR37
Molecular classification
G protein-coupled receptor, Class A GPCR, Rhodopsin-like GPCR
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Overview

G protein-coupled receptor 37 (GPR37) is a Class A GPCR primarily expressed in the central nervous system, particularly in neurons and glia. It functions in oligodendrocyte differentiation, CNS myelination, and neuroprotection through interactions with prosaposin and osteocalcin. GPR37 primarily couples to Gi/o proteins, inhibiting cAMP production and activating MAPK/ERK pathways. It has been implicated in Parkinson’s disease, cancer, stroke and multiple sclerosis. The long N-terminal domain undergoes rapid metalloprotease-mediated cleavage; the cleaved ectodomain is shed into the extracellular space.

Other names
Prosaposin receptorPael-R
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Mechanism of action

Gi/o protein activation, inhibition of adenylyl cyclase, activation of MAPK/ERK pathway, β-arrestin recruitment

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Biological functions

Signal transductionOligodendrocyte differentiationCNS myelinationNeuroprotectionWnt/β-catenin signaling modulation
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Disease associations

Parkinson’s diseaseCancerLung adenocarcinomaStrokeMultiple Sclerosis
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Safety considerations

Overexpression or misfolding can be cytotoxic if parkin is deficient or mutated.Potential off-target effects due to widespread CNS expression.

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