The mutation-mediated overexpression of epidermal growth factor receptor tyrosine kinase(EGFR TK)and its activation play an important role in the cellular proliferation and epithelial tumorigenesis.A series of inhibit...The mutation-mediated overexpression of epidermal growth factor receptor tyrosine kinase(EGFR TK)and its activation play an important role in the cellular proliferation and epithelial tumorigenesis.A series of inhibitors targeting the intracellular tyrosine kinase(TK)domain of EGFR have been developed and applied to clinical practice.Although these inhibitors safely and effectively restrain tumor cell proliferation and prolong survival in some patients,acquired resistance ultimately arises.DNA mutations contribute to druginduced cancer-cell resistance.展开更多
基金This work was supported by the National Institutes of Health[R01CA073764 to B.H.S.,R50CA211397 to L.Z.].
文摘The mutation-mediated overexpression of epidermal growth factor receptor tyrosine kinase(EGFR TK)and its activation play an important role in the cellular proliferation and epithelial tumorigenesis.A series of inhibitors targeting the intracellular tyrosine kinase(TK)domain of EGFR have been developed and applied to clinical practice.Although these inhibitors safely and effectively restrain tumor cell proliferation and prolong survival in some patients,acquired resistance ultimately arises.DNA mutations contribute to druginduced cancer-cell resistance.