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Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S† †Electronic supplementary information (ESI) available. CCDC 1876852. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c9sc03445e

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We present inhibitors of drug resistant mutants of EGFR including T790M and C797S. In addition, we present the first X-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR… Click to show full abstract

We present inhibitors of drug resistant mutants of EGFR including T790M and C797S. In addition, we present the first X-ray crystal structures of covalent inhibitors in complex with C797S-mutated EGFR to gain insight into their binding mode.

Keywords: osimertinib resistant; c797s; t790m c797s; esi; inhibition osimertinib

Journal Title: Chemical Science
Year Published: 2019

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