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a(CHEBI:gefitinib) =| kin(p(HGNC:EGFR))
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Approximately 61,000 statements.
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A multitude of synthetic tyrosine kinase inhibitors have been developed and screened for potential preclinical activity, most of which reversibly compete with ATP for binding to the enzyme's intracellular catalytic domain. The quinazoline derivatives ZD1839 (gefitinib, Iressa) and OSI- 774 (erlotinib, Tarceva) appear to be the most promising to date. ZD1839 is a synthetic anilinoquinazoline [4-(3-chloro-4- fluoroanilino)-7-methoxy-6-(3-morpholinopropoxy) quinazoline] that inhibits the EGFR tyrosine kinase, resulting in G1 cell cycle arrest and upregulation of the p27KIP1 cyclin dependent kinase inhibitor [88-91]
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