Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site
Günther, Marcel, Lategahn, Jonas, Juchum, Michael, Döring, Eva, Keul, Marina, Engel, Julian, Tumbrink, Hannah L, Rauh, Daniel, Laufer, Stefan
Published in Journal of medicinal chemistry (13.07.2017)
Published in Journal of medicinal chemistry (13.07.2017)
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Journal Article
Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor
Tomassi, Stefano, Lategahn, Jonas, Engel, Julian, Keul, Marina, Tumbrink, Hannah L, Ketzer, Julia, Mühlenberg, Thomas, Baumann, Matthias, Schultz-Fademrecht, Carsten, Bauer, Sebastian, Rauh, Daniel
Published in Journal of medicinal chemistry (23.03.2017)
Published in Journal of medicinal chemistry (23.03.2017)
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Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors
Plenker, Dennis, Riedel, Maximilian, Brägelmann, Johannes, Dammert, Marcel A, Chauhan, Rakhee, Knowles, Phillip P, Lorenz, Carina, Keul, Marina, Bührmann, Mike, Pagel, Oliver, Tischler, Verena, Scheel, Andreas H, Schütte, Daniel, Song, Yanrui, Stark, Justina, Mrugalla, Florian, Alber, Yannic, Richters, André, Engel, Julian, Leenders, Frauke, Heuckmann, Johannes M, Wolf, Jürgen, Diebold, Joachim, Pall, Georg, Peifer, Martin, Aerts, Maarten, Gevaert, Kris, Zahedi, René P, Buettner, Reinhard, Shokat, Kevan M, McDonald, Neil Q, Kast, Stefan M, Gautschi, Oliver, Thomas, Roman K, Sos, Martin L
Published in Science translational medicine (14.06.2017)
Published in Science translational medicine (14.06.2017)
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Analyzing Kinase Similarity in Small Molecule and Protein Structural Space to Explore the Limits of Multi-Target Screening
Schmidt, Denis, Scharf, Magdalena M, Sydow, Dominique, Aßmann, Eva, Martí-Solano, Maria, Keul, Marina, Volkamer, Andrea, Kolb, Peter
Published in Molecules (Basel, Switzerland) (26.01.2021)
Published in Molecules (Basel, Switzerland) (26.01.2021)
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Characterization of Covalent-Reversible EGFR Inhibitors
Smith, Steven, Keul, Marina, Engel, Julian, Basu, Debjit, Eppmann, Simone, Rauh, Daniel
Published in ACS omega (30.04.2017)
Published in ACS omega (30.04.2017)
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Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
Fassunke, Jana, Müller, Fabienne, Keul, Marina, Michels, Sebastian, Dammert, Marcel A., Schmitt, Anna, Plenker, Dennis, Lategahn, Jonas, Heydt, Carina, Brägelmann, Johannes, Tumbrink, Hannah L., Alber, Yannic, Klein, Sebastian, Heimsoeth, Alena, Dahmen, Ilona, Fischer, Rieke N., Scheffler, Matthias, Ihle, Michaela A., Priesner, Vanessa, Scheel, Andreas H., Wagener, Svenja, Kron, Anna, Frank, Konrad, Garbert, Katia, Persigehl, Thorsten, Püsken, Michael, Haneder, Stefan, Schaaf, Bernhard, Rodermann, Ernst, Engel-Riedel, Walburga, Felip, Enriqueta, Smit, Egbert F., Merkelbach-Bruse, Sabine, Reinhardt, H. Christian, Kast, Stefan M., Wolf, Jürgen, Rauh, Daniel, Büttner, Reinhard, Sos, Martin L.
Published in Nature communications (07.11.2018)
Published in Nature communications (07.11.2018)
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Overcoming EGFR G724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors
Fassunke, Jana, Müller, Fabienne, Keul, Marina, Michels, Sebastian, Dammert, Marcel A, Schmitt, Anna, Plenker, Dennis, Lategahn, Jonas, Heydt, Carina, Brägelmann, Johannes, Tumbrink, Hannah L, Alber, Yannic, Klein, Sebastian, Heimsoeth, Alena, Dahmen, Ilona, Fischer, Rieke N, Scheffler, Matthias, Ihle, Michaela A, Priesner, Vanessa, Scheel, Andreas H, Wagener, Svenja, Kron, Anna, Konrad, Frank, Garbert, Katia, Persigehl, Thorsten, Püsken, Michael, Haneder, Stefan, Schaaf, Bernhard, Rodermann, Ernst, Engel-Riedel, Walburga, Felip, Enriqueta, Smit, Egbert F, Merkelbach-Bruse, Sabine, Reinhardt, H Christian, Kast, Stefan M, Wolf, Jürgen, Rauh, Daniel, Büttner, Reinhard, Sos, Martin L
Published in Nature communications (01.11.2018)
Published in Nature communications (01.11.2018)
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Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR
Engel, Julian, Becker, Christian, Lategahn, Jonas, Keul, Marina, Ketzer, Julia, Mühlenberg, Thomas, Kollipara, Laxmikanth, Schultz-Fademrecht, Carsten, Zahedi, René P., Bauer, Sebastian, Rauh, Daniel
Published in Angewandte Chemie International Edition (26.08.2016)
Published in Angewandte Chemie International Edition (26.08.2016)
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Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach
Engel, Julian, Richters, André, Getlik, Matthäus, Tomassi, Stefano, Keul, Marina, Termathe, Martin, Lategahn, Jonas, Becker, Christian, Mayer-Wrangowski, Svenja, Grütter, Christian, Uhlenbrock, Niklas, Krüll, Jasmin, Schaumann, Niklas, Eppmann, Simone, Kibies, Patrick, Hoffgaard, Franziska, Heil, Jochen, Menninger, Sascha, Ortiz-Cuaran, Sandra, Heuckmann, Johannes M., Tinnefeld, Verena, Zahedi, René P., Sos, Martin L., Schultz-Fademrecht, Carsten, Thomas, Roman K., Kast, Stefan M., Rauh, Daniel
Published in Journal of medicinal chemistry (10.09.2015)
Published in Journal of medicinal chemistry (10.09.2015)
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Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors
Lategahn, Jonas, Tumbrink, Hannah L., Schultz-Fademrecht, Carsten, Heimsoeth, Alena, Werr, Lisa, Niggenaber, Janina, Keul, Marina, Parmaksiz, Fatma, Baumann, Matthias, Menninger, Sascha, Zent, Eldar, Landel, Ina, Weisner, Jörn, Jeyakumar, Kirujan, Heyden, Leonie, Russ, Nicole, Müller, Fabienne, Lorenz, Carina, Brägelmann, Johannes, Spille, Inga, Grabe, Tobias, Müller, Matthias P., Heuckmann, Johannes M., Klebl, Bert M., Nussbaumer, Peter, Sos, Martin L., Rauh, Daniel
Published in Journal of medicinal chemistry (12.05.2022)
Published in Journal of medicinal chemistry (12.05.2022)
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RASPELD to Perform High‐End Screening in an Academic Environment toward the Development of Cancer Therapeutics
Wolle, Patrik, Weisner, Jörn, Keul, Marina, Landel, Ina, Lategahn, Jonas, Rauh, Daniel
Published in ChemMedChem (08.10.2018)
Published in ChemMedChem (08.10.2018)
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Targeting Her2-insYVMA with Covalent InhibitorsA Focused Compound Screening and Structure-Based Design Approach
Lategahn, Jonas, Hardick, Julia, Grabe, Tobias, Niggenaber, Janina, Jeyakumar, Kirujan, Keul, Marina, Tumbrink, Hannah L, Becker, Christian, Hodson, Luke, Kirschner, Tonia, Klövekorn, Philip, Ketzer, Julia, Baumann, Matthias, Terheyden, Susanne, Unger, Anke, Weisner, Jörn, Müller, Matthias P, van Otterlo, Willem A. L, Bauer, Sebastian, Rauh, Daniel
Published in Journal of medicinal chemistry (22.10.2020)
Published in Journal of medicinal chemistry (22.10.2020)
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Inhibition of osimertinib-resistant epidermal growth factor receptor EGFR-T790M/C797S
Lategahn, Jonas, Keul, Marina, Klövekorn, Philip, Tumbrink, Hannah L, Niggenaber, Janina, Müller, Matthias P, Hodson, Luke, Flaßhoff, Maren, Hardick, Julia, Grabe, Tobias, Engel, Julian, Schultz-Fademrecht, Carsten, Baumann, Matthias, Ketzer, Julia, Mühlenberg, Thomas, Hiller, Wolf, Günther, Georgia, Unger, Anke, Müller, Heiko, Heimsoeth, Alena, Golz, Christopher, Blank-Landeshammer, Bernhard, Kollipara, Laxmikanth, Zahedi, René P, Strohmann, Carsten, Hengstler, Jan G, van Otterlo, Willem A. L, Bauer, Sebastian, Rauh, Daniel
Published in Chemical science (Cambridge) (14.12.2019)
Published in Chemical science (Cambridge) (14.12.2019)
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Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor
Engel, Julian, Smith, Steven, Lategahn, Jonas, Tumbrink, Hannah L, Goebel, Lisa, Becker, Christian, Hennes, Elisabeth, Keul, Marina, Unger, Anke, Müller, Heiko, Baumann, Matthias, Schultz-Fademrecht, Carsten, Günther, Georgia, Hengstler, Jan G, Rauh, Daniel
Published in Journal of medicinal chemistry (28.09.2017)
Published in Journal of medicinal chemistry (28.09.2017)
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Targeting EGFR Ex20 mutant lung cancer with the wild type sparing kinase inhibitor PRB001
Sos, Martin L., Tumbrink, Hannah Lea, Schultz-Fademrecht, Carsten, Lategahn, Jonas, Keul, Marina, Niggenaber, Janina, Heimsoeth, Alena, Baumann, Matthias, Werr, Lisa Hanna, Degenhart, Carsten, Menninger, Sascha, Heuckmann, Johannes M, Thomas, Roman K., Rauh, Daniel, Klebl, Bert
Published in Journal of clinical oncology (20.05.2019)
Published in Journal of clinical oncology (20.05.2019)
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Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
Kaitsiotou, Helena, Keul, Marina, Hardick, Julia, Mühlenberg, Thomas, Ketzer, Julia, Ehrt, Christiane, Krüll, Jasmin, Medda, Federico, Koch, Oliver, Giordanetto, Fabrizio, Bauer, Sebastian, Rauh, Daniel
Published in Journal of medicinal chemistry (09.11.2017)
Published in Journal of medicinal chemistry (09.11.2017)
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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
Lategahn, Jonas, Keul, Marina, Klövekorn, Philip, Tumbrink, Hannah L., Niggenaber, Janina, Müller, Matthias P., Hodson, Luke, Flaßhoff, Maren, Hardick, Julia, Grabe, Tobias, Engel, Julian, Schultz-Fademrecht, Carsten, Baumann, Matthias, Ketzer, Julia, Mühlenberg, Thomas, Hiller, Wolf, Günther, Georgia, Unger, Anke, Müller, Heiko, Heimsoeth, Alena, Golz, Christopher, Blank-Landeshammer, Bernhard, Kollipara, Laxmikanth, Zahedi, René P., Strohmann, Carsten, Hengstler, Jan G., van Otterlo, Willem A. L., Bauer, Sebastian, Rauh, Daniel
Published in Chemical science (Cambridge) (04.10.2019)
Published in Chemical science (Cambridge) (04.10.2019)
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