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The epidermal growth factor receptor (EGFR, erbB1, HER1) has been well validated as a molecular target in anticancer drug discovery.In non-small cell lung cancer patients (NSCLCs) harboring active mutations in the EGFR tyrosine kinase domain (i.e.L858R and del E746_A750) the first generation inhibitors, gefinitib and erlotinib have achieved significant clinical benefits but emerging acquired resistance to them has become a major clinical challenge.