Target intelligence / Profile preview

G protein-coupled receptor 27 (GPR27)

Target
GPR27
Molecular classification
G protein-coupled receptor, Orphan receptor, Transmembrane receptor, Class A (Rhodopsin-like) GPCR
01

Overview

G protein-coupled receptor 27 (GPR27) is an orphan Class A (Rhodopsin-like) G protein-coupled receptor highly conserved across vertebrates and predominantly expressed in the central nervous system, particularly in brain regions such as the hippocampal dentate gyrus and hypothalamus[2][4][7][8]. GPR27 is part of the "Super conserved receptor expressed in brain" (SREB) family, including SREB1 (GPR27), SREB2 (GPR85), and SREB3 (GPR173)[2][5]. No endogenous ligands have been identified, and its precise physiological and pathological roles remain undefined. Recent evidence links GPR27 to processes such as neural plasticity, neurodevelopmental disorders, and possibly insulin secretion, but functional studies are limited[4][8]. Two selective surrogate agonists have been discovered that activate β-arrestin recruitment, but not classical G protein pathways[3]. No established drugs target GPR27, and further research is needed to clarify its disease relevance and therapeutic utility.

Other names
Super conserved receptor expressed in brain 1SREB1Probable G-protein coupled receptor 27Orphan GPCRGPR27_HUMANQ9NS67
02

Mechanism of action

For surrogate agonists: β-arrestin 2 recruitment (no evidenced G protein activation for these compounds)[3]

03

Biological functions

Signal transductionPotential role in neural plasticityExpressed in central nervous system, especially in the brain
04

Disease associations

Neurodevelopmental disorders (e.g., associated with autism spectrum disorder and blepharophimosis due to chromosomal deletion including GPR27)Possible involvement in metabolic regulation (linked to insulin secretion in preliminary studies)
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Safety considerations

Lack of known endogenous ligand hampers therapeutic development and safety characterizationBiological function and systemic effects remain poorly understood, limiting clinical development
06

Interacting drugs

N-[4-(anilinocarbonyl)phenyl]-2,4-dichlorobenzamide (ChemBridge ID5128535)

1 more in the full profile.

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