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Target intelligence / Profile preview
Adhesion G protein-coupled receptor A2 (ADGRA2)
- Target
- ADGRA2
- Molecular classification
- G protein-coupled receptor, Adhesion GPCR family member, Transmembrane signaling receptor
01
Overview
Adhesion G protein-coupled receptor A2 (ADGRA2), also known as GPR124, is a member of the adhesion GPCR family characterized by a long extracellular region and a 7-transmembrane domain connected via a GAIN domain. ADGRA2 is primarily expressed in endothelial cells of the brain, where it interacts with RECK to mediate selective responses to Wnt7A and Wnt7B signals, crucial for canonical Wnt signaling. This facilitates CNS angiogenesis, endothelial cell migration, and the establishment and maintenance of the blood-brain barrier. ADGRA2 is upregulated in various cancers and is predicted to play a role in neurovascular development, making it relevant for cancer biology and brain development. No approved drugs currently target ADGRA2, but its restricted expression profile and disease association identify it as a candidate for future therapeutic research.
- Other names
- GPR124KIAA1531TEM5DKFZp434C211DKFZp434J0911FLJ14390G-protein coupled receptor 124tumor endothelial marker 5
02
Mechanism of action
Drugs would presumably affect Wnt signaling modulation, endothelial cell migration, or blood-brain barrier integrity, but specific mechanisms for therapeutics are not established
03
Biological functions
Signal transductionRegulation of canonical Wnt signaling pathwayEndothelial cell sprouting and migrationBlood-brain barrier formation and maintenanceCell adhesion
04
Disease associations
Cancer (e.g., glioma susceptibility, hematologic cancer)Brain development disorders (e.g., angiogenic deficiencies in CNS)Potential involvement in neuroinvasive virus entry
05
Safety considerations
Therapeutic targeting may affect vascular development and blood-brain barrier function, potentially leading to CNS or vascular side effectsSpecificity and off-target effects represent notable challenges
06
Interacting drugs
None clearly documented in publicly available sources. No approved drugs directly targeting ADGRA2 (GPR124) as of the current date; research is ongoing
07
Biomarkers
Overexpression in tumor endothelium (e.g., gliomas) may serve as a biomarker for disease or therapeutic response"tumor endothelial marker 5" refers to its use as a marker in cancer tissue
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