The erbB Family: Targets for Therapeutic Development Against Cancer and Therapeutic Strategies Using Monoclonal Antibodies and Tyrosine Kinase Inhibitors

摘要: The overexpression and aberrant function of members the erbB family receptors, particularly erbB1 (also known as epidermal growth factor receptor), its ligands in many human cancers have provided a rationale for targeting this signaling network with novel approaches. is selective target inhibiting because activation often confers proliferative advantage. Activation tyrosine kinase provides signals that drive dysregulated proliferation, invasion, metastasis, angiogenesis, cell survival, inhibition has potential both treatment prevention these malignancies. Based on structure erbB1, two therapeutic strategies been developed. first uses monoclonal antibodies (MAbs) generated against receptor's ligand-binding extracellular domain. These MAbs block binding receptor-activating ligands, and, some cases, can induce receptor endocytosis downregulation. second small molecules com...