Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S

• DOI: 10.1039/c9sc03445e
• Publication Date: 2019-10-04T09:23:34Z
• Authors: Jonas Lategahn; Marina Keul; Philip Klövekorn; Hannah L. Tumbrink; Janina Niggenaber; Matthias P. Müller; Luke Hodson; Maren Flaßhoff; Julia Hardick; Tobias Grabe; Julian Engel; Carsten Schultz-F...; Matthias Baumann; Julia Ketzer; Thomas Mühlenberg; Wolf Hiller; Georgia Günther; Anke Unger; Heiko Müller; Alena Heimsoeth; Christopher Golz; Bernhard Blank-La...; Laxmikanth Kollipara; René P. Zahedi; Carsten Strohmann; Jan G. Hengstler; Willem A. L. van ...; Sebastian Bauer; Daniel Rauh
• Keywords: Osimertinib; T790M; EGFR Inhibitors

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