... result in repositioning of critical residues surrounding the ATP-binding cleft of the tyrosine kinase domain of the receptor and therebystabilize the interaction with EGF-TKIs, leading to anincrease ... the tyrosine kinase activity of EGFR (EGFR-TKIs), gefiti-nib and erlotinib, compete with ATP for binding to the tyrosine kinase pocket of the receptor, therebyinhibiting receptor tyrosine kinase ... and small-molecule tyrosine kinase inhibitors, such as gefitinib and erlotinib, whichtarget the intracellular tyrosine kinase domain of the EGFR. Furthermore,recent clinical and laboratory studies...