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Target intelligence / Profile preview
Ephrin type-A Receptor EphA2 (EphA2)
- Target
- EphA2
- Molecular classification
- Receptor tyrosine kinase, Ephrin receptor subfamily
01
Overview
Ephrin type-A receptor 2 (EphA2) is a receptor tyrosine kinase that binds primarily to membrane-bound ephrin-A ligands on adjacent cells, mediating contact-dependent bidirectional signaling. It plays a role in various developmental processes and is implicated in cancer progression, viral entry, and other diseases. Overexpression or dysregulation is observed in many cancers. EPHA2 mRNA levels are modulated by natural antisense transcripts. It interacts with multiple intracellular signaling molecules upon activation.
- Other names
- Epithelial cell kinase (ECK)Tyrosine-protein kinase receptor ECKMPK-5SEK-2Myk2
02
Mechanism of action
EphA2 activation leads to complex signaling cascades including Rho GTPases activation, MAP kinases pathway activation, PI3K/AKT pathway modulation, and Src family kinases involvement. Acts through forward and reverse signaling.
03
Biological functions
Cell adhesionCell migrationCell proliferationCell differentiationCell survivalNervous system developmentEmbryonic lens and kidney developmentMammary epithelial branching morphogenesisBone homeostasisVascular developmentTissue boundary formation
04
Disease associations
Cancer (various types)Viral infection (KSHV)CataractsDevelopmental disorders
05
Safety considerations
Potential for off-target effects due to promiscuous ligand bindingTumor-specific expression variabilityResistance mechanisms to targeted therapies
06
Interacting drugs
Doxazosin
1 more in the full profile.
07
Biomarkers
EPHA2 expression levels in tumors (prognostic/predictive)EPHA2 mRNA levels in breast cancer subtypes
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