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Target intelligence / Profile preview
G protein-coupled receptor 65 (GPR65)
- Target
- GPR65
- Molecular classification
- G protein-coupled receptor, GPCR, Proton-sensing GPCR
01
Overview
GPR65 is a proton-sensing G protein-coupled receptor predominantly expressed in lymphoid tissues, retina, and vagal afferents. It is activated by acidic extracellular pH, leading to increased intracellular cAMP via Gs protein activation. GPR65 plays a role in immune modulation, cardioprotection post-myocardial infarction, neuroprotection in the retina and central nervous system, and other physiological processes. It is implicated in diseases such as multiple sclerosis, inflammatory diseases, myocardial infarction, retinal degeneration, depression, and potentially cancer.
- Other names
- Psychosine receptorT-cell death-associated gene 8 proteinTDAG8hTDAG8
02
Mechanism of action
Gs protein activation leading to increased cAMP production
03
Biological functions
Immune modulationCardioprotectionNeuroprotectionSignal transductionRegulation of cytokine productionRegulation of immune cell differentiationpH sensingInhibition of osteoclastic bone resorptionNutrient sensingGut motility regulation
04
Disease associations
Multiple sclerosisInflammatory diseasesColitisMyocardial infarctionRetinal degenerative diseasesDepressionCancer
05
Safety considerations
Potential for off-target effects due to broad tissue distributionComplex role in immune modulation requiring careful consideration of therapeutic context
06
Interacting drugs
BTB09089
1 more in the full profile.
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