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Target intelligence / Profile preview
G protein-coupled receptor 52 (GPR52)
- Target
- GPR52
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor, Class-A GPCR, Rhodopsin-like receptors
01
Overview
GPR52 is a class-A orphan G protein-coupled receptor (GPCR) primarily expressed in the brain, especially the striatum and nucleus accumbens. It couples to Gs/olf proteins, increasing intracellular cAMP. Its signaling modulates locomotor activity and is implicated in neuropsychiatric conditions like Huntington's disease and schizophrenia. It features an extracellular loop 2 (ECL2) that acts as a built-in agonist, conferring high basal activity. While no endogenous ligand is known, synthetic agonists binding to a unique side pocket near TM1/TM2/TM7/ECL2 close to the extracellular surface has been observed.
02
Mechanism of action
Gs/olf protein activation, increased cAMP production
03
Biological functions
Signal transductionRegulation of locomotor activityModulation of dopamine pathwaysModulation of NMDA receptor pathwaysModulation of adenosine A2A receptor pathways
04
Disease associations
Neurodegenerative diseaseHuntington's diseasePsychiatric disordersSchizophrenia
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