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Tyrosine-protein kinase EphA3 is a receptor tyrosine kinase belonging to the ephrin receptor subfamily, encoded by the EPHA3 gene located on chromosome 3p11.2. The receptor has an extracellular region with a cysteine-rich domain and fibronectin type III repeats, a transmembrane region, and an intracellular tyrosine kinase domain. EphA3 primarily binds ephrin-A family ligands, mediating repulsive and adhesive cell signaling important in embryonic tissue patterning, cell positioning, and nervous system development. In adults, EphA3 is sparsely expressed in most tissues but is overexpressed in various malignancies, making it a therapeutic target for cancer drug development, particularly monoclonal antibodies and kinase inhibitors[5][12][13][16][15][14].
Inhibition of kinase activity Disruption of ligand (ephrin) binding Modulation of cell signaling to inhibit tumor cell migration, proliferation, and survival Antibody-dependent cellular cytotoxicity (for some monoclonal antibodies)
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