Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
Kim, Dongsung, Herdeis, Lorenz, Rudolph, Dorothea, Zhao, Yulei, Böttcher, Jark, Vides, Alberto, Ayala-Santos, Carlos I., Pourfarjam, Yasin, Cuevas-Navarro, Antonio, Xue, Jenny Y., Mantoulidis, Andreas, Bröker, Joachim, Wunberg, Tobias, Schaaf, Otmar, Popow, Johannes, Wolkerstorfer, Bernhard, Kropatsch, Katrin Gabriele, Qu, Rui, de Stanchina, Elisa, Sang, Ben, Li, Chuanchuan, McConnell, Darryl B., Kraut, Norbert, Lito, Piro
Published in Nature (London) (06.07.2023)
Published in Nature (London) (06.07.2023)
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Journal Article
Discovery of Novel Spiro[3H‑indole-3,2′-pyrrolidin]-2(1H)‑one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2–p53 Interaction
Gollner, Andreas, Rudolph, Dorothea, Arnhof, Heribert, Bauer, Markus, Blake, Sophia M, Boehmelt, Guido, Cockroft, Xiao-Ling, Dahmann, Georg, Ettmayer, Peter, Gerstberger, Thomas, Karolyi-Oezguer, Jale, Kessler, Dirk, Kofink, Christiane, Ramharter, Juergen, Rinnenthal, Jörg, Savchenko, Alexander, Schnitzer, Renate, Weinstabl, Harald, Weyer-Czernilofsky, Ulrike, Wunberg, Tobias, McConnell, Darryl B
Published in Journal of medicinal chemistry (23.11.2016)
Published in Journal of medicinal chemistry (23.11.2016)
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Journal Article
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Journal Article
Direct NMR Probing of Hydration Shells of Protein Ligand Interfaces and Its Application to Drug Design
Geist, Leonhard, Mayer, Moriz, Cockcroft, Xiao-Ling, Wolkerstorfer, Bernhard, Kessler, Dirk, Engelhardt, Harald, McConnell, Darryl B, Konrat, Robert
Published in Journal of medicinal chemistry (09.11.2017)
Published in Journal of medicinal chemistry (09.11.2017)
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Journal Article
Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS
Hodges, Timothy R, Abbott, Jason R, Little, Andrew J, Sarkar, Dhruba, Salovich, James M, Howes, Jennifer E, Akan, Denis T, Sai, Jiqing, Arnold, Allison L, Browning, Carrie, Burns, Michael C, Sobolik, Tammy, Sun, Qi, Beesetty, Yugandhar, Coker, Jesse A, Scharn, Dirk, Stadtmueller, Heinz, Rossanese, Olivia W, Phan, Jason, Waterson, Alex G, McConnell, Darryl B, Fesik, Stephen W
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Journal Article
Targeting Son of Sevenless 1: The pacemaker of KRAS
Kessler, Dirk, Gerlach, Daniel, Kraut, Norbert, McConnell, Darryl B.
Published in Current opinion in chemical biology (01.06.2021)
Published in Current opinion in chemical biology (01.06.2021)
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Journal Article
Stopping the beating heart of cancer: KRAS reviewed
Herdeis, Lorenz, Gerlach, Daniel, McConnell, Darryl B., Kessler, Dirk
Published in Current opinion in structural biology (01.12.2021)
Published in Current opinion in structural biology (01.12.2021)
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Journal Article
Transforming targeted cancer therapy with PROTACs: A forward-looking perspective
Farnaby, William, Koegl, Manfred, McConnell, Darryl B., Ciulli, Alessio
Published in Current opinion in pharmacology (01.04.2021)
Published in Current opinion in pharmacology (01.04.2021)
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Journal Article
The hanging heart: How KRAS lures its prey to the membrane
Kessler, Dirk, McConnell, Darryl B.
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2020)
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2020)
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Journal Article
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
Farnaby, William, Koegl, Manfred, Roy, Michael J., Whitworth, Claire, Diers, Emelyne, Trainor, Nicole, Zollman, David, Steurer, Steffen, Karolyi-Oezguer, Jale, Riedmueller, Carina, Gmaschitz, Teresa, Wachter, Johannes, Dank, Christian, Galant, Michael, Sharps, Bernadette, Rumpel, Klaus, Traxler, Elisabeth, Gerstberger, Thomas, Schnitzer, Renate, Petermann, Oliver, Greb, Peter, Weinstabl, Harald, Bader, Gerd, Zoephel, Andreas, Weiss-Puxbaum, Alexander, Ehrenhöfer-Wölfer, Katharina, Wöhrle, Simon, Boehmelt, Guido, Rinnenthal, Joerg, Arnhof, Heribert, Wiechens, Nicola, Wu, Meng-Ying, Owen-Hughes, Tom, Ettmayer, Peter, Pearson, Mark, McConnell, Darryl B., Ciulli, Alessio
Published in Nature chemical biology (01.07.2019)
Published in Nature chemical biology (01.07.2019)
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Journal Article
PI by NMR: Probing CH–π Interactions in Protein–Ligand Complexes by NMR Spectroscopy
Platzer, Gerald, Mayer, Moriz, Beier, Andreas, Brüschweiler, Sven, Fuchs, Julian E., Engelhardt, Harald, Geist, Leonhard, Bader, Gerd, Schörghuber, Julia, Lichtenecker, Roman, Wolkerstorfer, Bernhard, Kessler, Dirk, McConnell, Darryl B., Konrat, Robert
Published in Angewandte Chemie International Edition (24.08.2020)
Published in Angewandte Chemie International Edition (24.08.2020)
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Journal Article
Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions
Popow, Johannes, Arnhof, Heribert, Bader, Gerd, Berger, Helmut, Ciulli, Alessio, Covini, David, Dank, Christian, Gmaschitz, Teresa, Greb, Peter, Karolyi-Özguer, Jale, Koegl, Manfred, McConnell, Darryl B, Pearson, Mark, Rieger, Maria, Rinnenthal, Joerg, Roessler, Vanessa, Schrenk, Andreas, Spina, Markus, Steurer, Steffen, Trainor, Nicole, Traxler, Elisabeth, Wieshofer, Corinna, Zoephel, Andreas, Ettmayer, Peter
Published in Journal of medicinal chemistry (14.03.2019)
Published in Journal of medicinal chemistry (14.03.2019)
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Journal Article
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors
Engelhardt, Harald, Böse, Dietrich, Petronczki, Mark, Scharn, Dirk, Bader, Gerd, Baum, Anke, Bergner, Andreas, Chong, Eugene, Döbel, Sandra, Egger, Georg, Engelhardt, Christian, Ettmayer, Peter, Fuchs, Julian E, Gerstberger, Thomas, Gonnella, Nina, Grimm, Andreas, Grondal, Elisabeth, Haddad, Nizar, Hopfgartner, Barbara, Kousek, Roland, Krawiec, Mariusz, Kriz, Monika, Lamarre, Lyne, Leung, Joyce, Mayer, Moriz, Patel, Nitinchandra D, Simov, Biljana Peric, Reeves, Jonathan T, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Solca, Flavio, Stadtmüller, Heinz, Tan, Zhulin, Wunberg, Tobias, Zoephel, Andreas, McConnell, Darryl B
Published in Journal of medicinal chemistry (27.11.2019)
Published in Journal of medicinal chemistry (27.11.2019)
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Journal Article
Synthesis of a 13C-methylene-labeled isoleucine precursor as a useful tool for studying protein side-chain interactions and dynamics
Höfurthner, Theresa, Toscano, Giorgia, Kontaxis, Georg, Beier, Andreas, Mayer, Moriz, Geist, Leonhard, McConnell, Darryl B., Weinstabl, Harald, Lichtenecker, Roman, Konrat, Robert
Published in Journal of biomolecular NMR (01.03.2024)
Published in Journal of biomolecular NMR (01.03.2024)
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Journal Article
13 Cβ‐Valine and 13 Cγ‐Leucine Methine Labeling To Probe Protein Ligand Interaction
Toscano, Giorgia, Höfurthner, Theresa, Nagl, Benjamin, Beier, Andreas, Mayer, Moriz, Geist, Leonhard, McConnell, Darryl B., Weinstabl, Harald, Konrat, Robert, Lichtenecker, Roman J.
Published in Chembiochem : a European journal of chemical biology (15.03.2024)
Published in Chembiochem : a European journal of chemical biology (15.03.2024)
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Journal Article
Probing Protein–Ligand Methyl−π Interaction Geometries through Chemical Shift Measurements of Selectively Labeled Methyl Groups
Beier, Andreas, Platzer, Gerald, Höfurthner, Theresa, Ptaszek, Aleksandra L., Lichtenecker, Roman J., Geist, Leonhard, Fuchs, Julian E., McConnell, Darryl B., Mayer, Moriz, Konrat, Robert
Published in Journal of medicinal chemistry (08.08.2024)
Published in Journal of medicinal chemistry (08.08.2024)
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Journal Article
13Cβ‐Valine and 13Cγ‐Leucine Methine Labeling To Probe Protein Ligand Interaction
Toscano, Giorgia, Höfurthner, Theresa, Nagl, Benjamin, Beier, Andreas, Mayer, Moriz, Geist, Leonhard, McConnell, Darryl B., Weinstabl, Harald, Konrat, Robert, Lichtenecker, Roman J.
Published in Chembiochem : a European journal of chemical biology (15.03.2024)
Published in Chembiochem : a European journal of chemical biology (15.03.2024)
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Journal Article
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS
Ramharter, Juergen, Kessler, Dirk, Ettmayer, Peter, Hofmann, Marco H, Gerstberger, Thomas, Gmachl, Michael, Wunberg, Tobias, Kofink, Christiane, Sanderson, Michael, Arnhof, Heribert, Bader, Gerd, Rumpel, Klaus, Zöphel, Andreas, Schnitzer, Renate, Böttcher, Jark, O’Connell, Jonathan C, Mendes, Rachel L, Richard, David, Pototschnig, Nikolai, Weiner, Irene, Hela, Wolfgang, Hauer, Katja, Haering, Daniela, Lamarre, Lyne, Wolkerstorfer, Bernhard, Salamon, Christian, Werni, Patrick, Munico-Martinez, Silvia, Meyer, Reiner, Kennedy, Matthew D, Kraut, Norbert, McConnell, Darryl B
Published in Journal of medicinal chemistry (27.05.2021)
Published in Journal of medicinal chemistry (27.05.2021)
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Journal Article
Drugging all RAS isoforms with one pocket
Kessler, Dirk, Bergner, Andreas, Böttcher, Jark, Fischer, Gerhard, Döbel, Sandra, Hinkel, Melanie, Müllauer, Barbara, Weiss-Puxbaum, Alexander, McConnell, Darryl B
Published in Future medicinal chemistry (01.11.2020)
Published in Future medicinal chemistry (01.11.2020)
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