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Structure-Based Approach for the Discovery of Pyrrolo[3,2-<i>d</i>]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors

18 Dec 2012

Abstract excerpt

The epidermal growth factor receptor (EGFR) family plays a critical role in vital cellular processes and in various cancers. Known EGFR inhibitors exhibit distinct antitumor responses against the various EGFR mutants associated with nonsmall-cell lung cancer. The L858R mutation enhances clinical sensitivity to gefitinib and erlotinib as compared with wild type and reduces the relative sensitivity to lapatinib. In...

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PMID: 24900643
DOI: 10.1021/ml300327z

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