靶标信息
EGFR, epidermal growth factor receptor, is a receptor tyrosine kinases that signals in response to various growth factors. Overexpression has been linked to numerous types of cancer and EGFR is the target of both biological and small molecular therapeutics. EGFR is encoded by the EGFR gene located on chromosome 7 in humans. EGFR belongs to the HER/ERbB family of proteins that includes three other receptor tyrosine kinases, ERbB2, ERbB3, ERbB4. EGFR is a transmembrane receptor and binding of its cognate ligands such as EGF (Epidermal Growth Factor) and TGF alpha (Transforming Growth Factor alpha) to the extracellular domain leads to EGFR dimerization followed by autophosphorylation of the tyrosine residues in the cytoplasmic domain. Overexpression is observed in tumors of the head and neck, brain, bladder, stomach, breast, lung, endometrium, cervix, vulva, ovary, esophagus, stomach and in squamous cell carcinoma.
MET (cMET) is a receptor-like tyrosine kinase whose dysregulation has been linked to many types of human malignancies. After activation of the ligand, MET interacts with the PI3-kinase subunit PIK3R1, PLCG1, SRC, GRB2, and STAT3. There interactions lead to the activation of signaling cascades including RAS-ERK, PI3, kinase-AKT, and PLCgamma-PKC. MET plays a role in embryonic development including gastrulation, development of muscles and neurons, angiogenesis, and kidney formation. It also plays a role in adults including wound healing, organ regeneration, and tissue remodeling. MET has been linked to cancers including gastric, renal, and breast; therefore, making it a target for cancer therapeutics and diagnostic testing.