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The epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor gefitinib (ZD1839, Iressa) is approved for cancer treatment. We investigated whether gefitinib treatment can enhance human EGF (hEGF) uptake in vitro, thereby increasing the potential of hEGF as a vehicle for EGFR-targeted therapy.

Significant increase in hEGF uptake is correlated with formation of EGFR dimers induced by the EGFR tyrosine kinase inhibitor gefitinib