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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Nature Portfolio
2018
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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) |
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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 |
work_keys_str_mv |
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