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
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Lenguaje:EN
Publicado: Nature Portfolio 2018
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Acceso en línea:https://doaj.org/article/d0509a8e9f1241e6a692b9bd9e5d0a9b
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spelling oai:doaj.org-article:d0509a8e9f1241e6a692b9bd9e5d0a9b2021-12-02T15:33:46ZOvercoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors10.1038/s41467-018-07078-02041-1723https://doaj.org/article/d0509a8e9f1241e6a692b9bd9e5d0a9b2018-11-01T00:00:00Zhttps://doi.org/10.1038/s41467-018-07078-0https://doaj.org/toc/2041-1723Acquired 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.Jana FassunkeFabienne MüllerMarina KeulSebastian MichelsMarcel A. DammertAnna SchmittDennis PlenkerJonas LategahnCarina HeydtJohannes BrägelmannHannah L. TumbrinkYannic AlberSebastian KleinAlena HeimsoethIlona DahmenRieke N. FischerMatthias SchefflerMichaela A. IhleVanessa PriesnerAndreas H. ScheelSvenja WagenerAnna KronKonrad FrankKatia GarbertThorsten PersigehlMichael PüskenStefan HanederBernhard SchaafErnst RodermannWalburga Engel-RiedelEnriqueta FelipEgbert F. SmitSabine Merkelbach-BruseH. Christian ReinhardtStefan M. KastJürgen WolfDaniel RauhReinhard BüttnerMartin L. SosNature PortfolioarticleScienceQENNature Communications, Vol 9, Iss 1, Pp 1-13 (2018)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
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
Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
description 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.
format article
author 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
author_facet 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
author_sort Jana Fassunke
title Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
title_short Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
title_full Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
title_fullStr Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
title_full_unstemmed Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
title_sort overcoming egfr g724s-mediated osimertinib resistance through unique binding characteristics of second-generation egfr inhibitors
publisher Nature Portfolio
publishDate 2018
url https://doaj.org/article/d0509a8e9f1241e6a692b9bd9e5d0a9b
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