Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

Acquired resistance to targeted drugs remains a major clinical challenge in lung adenocarcinoma patients. Here, the authors show how the acquired EGFR G724S mutation induces resistance to third-generation EGFR inhibitors and why the mutant kinase remains susceptible to second-generation inhibitors....

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Autores principales: Jana Fassunke, Fabienne Müller, Marina Keul, Sebastian Michels, Marcel A. Dammert, Anna Schmitt, Dennis Plenker, Jonas Lategahn, Carina Heydt, Johannes Brägelmann, Hannah L. Tumbrink, Yannic Alber, Sebastian Klein, Alena Heimsoeth, Ilona Dahmen, Rieke N. Fischer, Matthias Scheffler, Michaela A. Ihle, Vanessa Priesner, Andreas H. Scheel, Svenja Wagener, Anna Kron, Konrad Frank, Katia Garbert, Thorsten Persigehl, Michael Püsken, Stefan Haneder, Bernhard Schaaf, Ernst Rodermann, Walburga Engel-Riedel, Enriqueta Felip, Egbert F. Smit, Sabine Merkelbach-Bruse, H. Christian Reinhardt, Stefan M. Kast, Jürgen Wolf, Daniel Rauh, Reinhard Büttner, Martin L. Sos
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2018
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Science
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Acceso en línea:https://doaj.org/article/d0509a8e9f1241e6a692b9bd9e5d0a9b
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Sumario:Acquired resistance to targeted drugs remains a major clinical challenge in lung adenocarcinoma patients. Here, the authors show how the acquired EGFR G724S mutation induces resistance to third-generation EGFR inhibitors and why the mutant kinase remains susceptible to second-generation inhibitors.

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