Eph receptor A2 (EPHA2)

Eph receptor A2 (EPHA2), originally identified as epithelial cell kinase (ECK), is a prominent member of the Ephrin receptor subfamily of receptor tyrosine kinases (RTKs) (Source: UniProt, Wikipedia). It is a transmembrane protein that mediates contact-dependent bidirectional signaling by interacting with membrane-bound ephrin-A ligands on adjacent cells (Source: NCBI, Sino Biological). EPHA2 plays a critical role in developmental processes such as angiogenesis, axon guidance, and tissue patterning (Source: BioVendor, ClinicalGate). In adult tissues, its expression is typically low and restricted to epithelial cells, but it is frequently overexpressed in various cancers, including glioblastoma, melanoma, and breast cancer, where it promotes tumor growth, metastasis, and drug resistance (Source: NIH, MDPI). Interestingly, EPHA2 exhibits a dual role in cancer: ligand-dependent forward signaling often acts as a tumor suppressor, while ligand-independent non-canonical signaling, driven by phosphorylation at Ser897, promotes malignancy (Source: NIH, MedChemExpress). Therapeutic strategies targeting EPHA2 include small-molecule kinase inhibitors, monoclonal antibodies, antibody-drug conjugates, and CAR-T cell therapies, though challenges remain regarding its complex signaling and expression in normal tissues (Source: NIH, Wikipedia).

Other names

Epithelial cell kinaseECKTyrosine-protein kinase receptor ECKEphrin type-A receptor 2ARCC2CTPACTPP1CTRCT6

Kinase inhibition, receptor degradation, ligand-binding blockade, and targeted cell killing via antibody-drug conjugates or CAR-T cells.