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Multiple tyrosine kinase receptors (RTKs) are a family of high-affinity cell surface receptors for polypeptide growth factors, cytokines, and hormones. They are single-pass transmembrane proteins with an extracellular ligand-binding domain, a transmembrane domain, and an intracellular tyrosine kinase domain. Ligand binding induces dimerization and autophosphorylation, activating downstream signaling pathways such as Ras/MAPK, PI3K/Akt, and PLCγ, which regulate cell proliferation, differentiation, survival, metabolism, and migration. Aberrant activation of RTKs is implicated in many cancers, making them major targets for therapeutic intervention with monoclonal antibodies and small-molecule inhibitors.
Inhibition of tyrosine kinase activity, blockade of ligand binding
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