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Target intelligence / Profile preview
G protein-coupled receptor 174 (GPR174)
- Target
- GPR174
- Molecular classification
- G protein-coupled receptor, Receptor, 7 transmembrane domain receptor, Orphan receptor
01
Overview
G protein-coupled receptor 174 (GPR174) is an orphan G protein-coupled receptor (GPCR) encoded by the GPR174 gene, most prominently expressed in immune tissues. It is structurally characterized by seven transmembrane alpha-helical domains typical of the GPCR superfamily. Functionally, GPR174 binds lysophosphatidylserine (LysoPS), mediating immune regulatory effects, including negative regulation of regulatory T-cell accumulation, suppression of interleukin-2 (IL-2) production in activated T cells, and modulation of B-cell and macrophage function. These effects are mediated primarily via G(12)/G(13) and G(q) G-protein signaling pathways, elevating cAMP and activating protein kinase A. GPR174 has been implicated as a genetic risk locus in autoimmune diseases such as Graves’ disease and may play roles in sepsis, adrenal cortical hypofunction, and hypertensive retinopathy. Currently, there are no approved drugs specifically targeting GPR174, but it is considered a potential therapeutic and immunomodulatory target due to its immune regulatory functions[2][3][7][9].
- Other names
- FKSG79LYPSR3GPCR17Probable G protein-coupled receptor 174
02
Mechanism of action
Agonism/antagonism at the G protein-coupled receptor 174 (emerging evidence for activity by lysophosphatidylserine and potentially chemokine CCL21 under testosterone stimulation) Modulation of intracellular cyclic AMP (cAMP) levels via G(12)/G(13) and G(q) pathways
03
Biological functions
Signal transductionImmune responseRegulation of T-cell activityRegulation of cytokine secretionInhibition of T-cell growth, proliferation, and differentiation
04
Disease associations
InflammationAutoimmune disease (e.g., risk locus for Graves' disease)Infection (role in sepsis)Potential role in hypertensive retinopathy and adrenal cortical hypofunction
05
Safety considerations
Modulation of immune cell function (especially T-lymphocyte and regulatory T-cell activity) may present risks of immune dysregulation or immunosuppression, but no specific safety signals are established due to lack of clinical pharmacology
06
Interacting drugs
None approved; no widely validated small molecule, biologic, or drug is currently annotated as interacting with GPR174 in standard drug databases
07
Biomarkers
None currently established or widely validated for patient selection or efficacy monitoring
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