Overview of epidermal growth factor receptor biology and its role as a therapeutic target in human neoplasia.

摘要: The ability of the epidermal growth factor receptor (EGFR) to transform epithelial cells, overexpression EGFR and its ligands in several human carcinomas, causal association network with accelerated tumor progression provided a rationale for targeting this signaling system tumor-selective strategies. Two these antireceptor approaches, both based on known structure/function EGFR, will be discussed. first strategy involved development humanized monoclonal antibodies against nonconserved receptor's extracellular domain. These block ligand binding can induce downregulation. second approach was generation adenosine triphosphate-mimetics that compete triphosphate kinase pocket disable transduce intracellular signals. Early clinical studies already suggest either alone or combination standard anticancer therapies, alter natural history EGFR-expressing cancers little toxicity tumor-bearing host.