Target intelligence / Profile preview

G protein-coupled receptor 68 (GPR68)

Target
GPR68
Molecular classification
G protein-coupled receptor, GPCR, Class A GPCR, Rhodopsin-like GPCR
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Overview

G protein-coupled receptor 68 (GPR68), also known as Ovarian cancer G-protein coupled receptor 1 (OGR1) or Sphingosylphosphorylcholine receptor, is a proton-sensing receptor that responds to changes in extracellular pH. It is involved in various biological activities, including inflammation, cardiovascular physiology, and tumor microenvironment modulation. GPR68 is expressed widely across tissues and is considered a potential drug target for inflammatory diseases and cancers characterized by acidic microenvironments.

Other names
OGR1Ovarian cancer G-protein coupled receptor 1Sphingosylphosphorylcholine receptor
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Mechanism of action

Acts as a proton-sensing receptor, responding to changes in extracellular pH and activating downstream signaling pathways, including cAMP/PKA/CREB signaling. May also be regulated by certain lipid molecules.

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Biological functions

Signal transductionProton sensingRegulation of inflammatory responsesRegulation of cell migrationCardiovascular physiology
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Disease associations

OsteoarthritisInflammationCancerTumor microenvironment modulationCardiovascular disease
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Safety considerations

Potential for off-target effects due to broad tissue expressionComplexity of downstream signaling pathways may lead to unpredictable effectsAcidosis-driven activation
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Biomarkers

GPR68 expression in cartilage as an indicator of osteoarthritis progression

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