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
The IGF1R/INSR Inhibitor BI 885578 Selectively Inhibits Growth of IGF2-Overexpressing Colorectal Cancer Tumors and Potentiates the Efficacy of Anti-VEGF Therapy
Sanderson, Michael P, Hofmann, Marco H, Garin-Chesa, Pilar, Schweifer, Norbert, Wernitznig, Andreas, Fischer, Stefan, Jeschko, Astrid, Meyer, Reiner, Moll, Jürgen, Pecina, Thomas, Arnhof, Heribert, Weyer-Czernilofsky, Ulrike, Zahn, Stephan K, Adolf, Günther R, Kraut, Norbert
Published in Molecular cancer therapeutics (01.10.2017)
Published in Molecular cancer therapeutics (01.10.2017)
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Journal Article
BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
Hofmann, Marco H, Gmachl, Michael, Ramharter, Juergen, Savarese, Fabio, Gerlach, Daniel, Marszalek, Joseph R, Sanderson, Michael P, Kessler, Dirk, Trapani, Francesca, Arnhof, Heribert, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Zoephel, Andreas, Fu, Szu-Chin, Teh, Jessica L, Böttcher, Jark, Pototschnig, Nikolai, Schachinger, Franziska, Schipany, Katharina, Lieb, Simone, Vellano, Christopher P, O'Connell, Jonathan C, Mendes, Rachel L, Moll, Jurgen, Petronczki, Mark, Heffernan, Timothy P, Pearson, Mark, McConnell, Darryl B, Kraut, Norbert
Published in Cancer discovery (01.01.2021)
Published in Cancer discovery (01.01.2021)
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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
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
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3
Böttcher, Jark, Dilworth, David, Reiser, Ulrich, Neumüller, Ralph A., Schleicher, Michael, Petronczki, Mark, Zeeb, Markus, Mischerikow, Nikolai, Allali-Hassani, Abdellah, Szewczyk, Magdalena M., Li, Fengling, Kennedy, Steven, Vedadi, Masoud, Barsyte-Lovejoy, Dalia, Brown, Peter J., Huber, Kilian V. M., Rogers, Catherine M., Wells, Carrow I., Fedorov, Oleg, Rumpel, Klaus, Zoephel, Andreas, Mayer, Moriz, Wunberg, Tobias, Böse, Dietrich, Zahn, Stephan, Arnhof, Heribert, Berger, Helmut, Reiser, Christoph, Hörmann, Alexandra, Krammer, Teresa, Corcokovic, Maja, Sharps, Bernadette, Winkler, Sandra, Häring, Daniela, Cockcroft, Xiao-Ling, Fuchs, Julian E., Müllauer, Barbara, Weiss-Puxbaum, Alexander, Gerstberger, Thomas, Boehmelt, Guido, Vakoc, Christopher R., Arrowsmith, Cheryl H., Pearson, Mark, McConnell, Darryl B.
Published in Nature chemical biology (01.08.2019)
Published in Nature chemical biology (01.08.2019)
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Journal Article
Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis
Weinstabl, Harald, Treu, Matthias, Rinnenthal, Joerg, Zahn, Stephan K, Ettmayer, Peter, Bader, Gerd, Dahmann, Georg, Kessler, Dirk, Rumpel, Klaus, Mischerikow, Nikolai, Savarese, Fabio, Gerstberger, Thomas, Mayer, Moriz, Zoephel, Andreas, Schnitzer, Renate, Sommergruber, Wolfgang, Martinelli, Paola, Arnhof, Heribert, Peric-Simov, Biljana, Hofbauer, Karin S, Garavel, Géraldine, Scherbantin, Yvonne, Mitzner, Sophie, Fett, Thomas N, Scholz, Guido, Bruchhaus, Jens, Burkard, Michelle, Kousek, Roland, Ciftci, Tuncay, Sharps, Bernadette, Schrenk, Andreas, Harrer, Christoph, Haering, Daniela, Wolkerstorfer, Bernhard, Zhang, Xuechun, Lv, Xiaobing, Du, Alicia, Li, Dongyang, Li, Yali, Quant, Jens, Pearson, Mark, McConnell, Darryl B
Published in Journal of medicinal chemistry (12.09.2019)
Published in Journal of medicinal chemistry (12.09.2019)
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Journal Article
Discovery of BI 7446: A Potent Cyclic Dinucleotide STING Agonist with Broad-Spectrum Variant Activity for the Treatment of Cancer
Kuttruff, Christian A., Fleck, Martin, Carotta, Sebastian, Arnhof, Heribert, Bretschneider, Tom, Dahmann, Georg, Gremel, Gabriela, Grube, Achim, Handschuh, Sandra, Heimann, Annekatrin, Hofmann, Marco H., Impagnatiello, Maria A., Nar, Herbert, Rast, Georg, Schaaf, Otmar, Schmidt, Esther, Oost, Thorsten
Published in Journal of medicinal chemistry (27.07.2023)
Published in Journal of medicinal chemistry (27.07.2023)
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Journal Article
Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Hofmann, Marco H, Mani, Rajeswaran, Engelhardt, Harald, Impagnatiello, Maria A, Carotta, Sebastian, Kerenyi, Marc, Lorenzo-Herrero, Seila, Böttcher, Jark, Scharn, Dirk, Arnhof, Heribert, Zoephel, Andreas, Schnitzer, Renate, Gerstberger, Thomas, Sanderson, Michael P, Rajgolikar, Girish, Goswami, Swagata, Vasu, Sumithira, Ettmayer, Peter, Gonzalez, Segundo, Pearson, Mark, McConnell, Darryl B, Kraut, Norbert, Muthusamy, Natarajan, Moll, Jürgen
Published in Molecular cancer therapeutics (01.04.2020)
Published in Molecular cancer therapeutics (01.04.2020)
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Journal Article
Combining SOS1 and MEK Inhibitors in a Murine Model of Plexiform Neurofibroma Results in Tumor Shrinkage
Jackson, Mark, Ahmari, Niousha, Wu, Jianqiang, Rizvi, Tilat A., Fugate, Elizabeth, Kim, Mi-OK, Dombi, Eva, Arnhof, Heribert, Boehmelt, Guido, Düchs, Matthias J., Long, Clive J., Maier, Udo, Trapani, Francesca, Hofmann, Marco H., Ratner, Nancy
Published in The Journal of pharmacology and experimental therapeutics (01.05.2023)
Published in The Journal of pharmacology and experimental therapeutics (01.05.2023)
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Journal Article
Targeting cancer with small-molecule pan-KRAS degraders
Popow, Johannes, Farnaby, William, Gollner, Andreas, Kofink, Christiane, Fischer, Gerhard, Wurm, Melanie, Zollman, David, Wijaya, Andre, Mischerikow, Nikolai, Hasenoehrl, Carina, Prokofeva, Polina, Arnhof, Heribert, Arce-Solano, Silvia, Bell, Sammy, Boeck, Georg, Diers, Emelyne, Frost, Aileen B, Goodwin-Tindall, Jake, Karolyi-Oezguer, Jale, Khan, Shakil, Klawatsch, Theresa, Koegl, Manfred, Kousek, Roland, Kratochvil, Barbara, Kropatsch, Katrin, Lauber, Arnel A, McLennan, Ross, Olt, Sabine, Peter, Daniel, Petermann, Oliver, Roessler, Vanessa, Stolt-Bergner, Peggy, Strack, Patrick, Strauss, Eva, Trainor, Nicole, Vetma, Vesna, Whitworth, Claire, Zhong, Siying, Quant, Jens, Weinstabl, Harald, Kuster, Bernhard, Ettmayer, Peter, Ciulli, Alessio
Published in Science (American Association for the Advancement of Science) (20.09.2024)
Published in Science (American Association for the Advancement of Science) (20.09.2024)
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Journal Article
Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors
Tarr, James C., Salovich, James M., Aichinger, Martin, Jeon, KyuOk, Veerasamy, Nagarathanam, Sensintaffar, John L., Arnhof, Heribert, Samwer, Matthias, Christov, Plamen P., Kim, Kwangho, Wunberg, Tobias, Schweifer, Norbert, Trapani, Francesca, Arnold, Allison, Martin, Florian, Zhao, Bin, Miriyala, Nagaraju, Sgubin, Danielle, Fogarty, Stuart, Moore, William J., Stott, Gordon M., Olejniczak, Edward T., Engelhardt, Harald, Rudolph, Dorothea, Lee, Taekyu, McConnell, Darryl B., Fesik, Stephen W.
Published in Journal of medicinal chemistry (05.08.2024)
Published in Journal of medicinal chemistry (05.08.2024)
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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 KRAS G12C 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
Abstract A030: Evaluation of phosphoprotein- and transcript-based pharmacodynamic biomarkers in pre-clinical studies of the novel SOS1::KRAS inhibitor BI-3406
Gerlach, Daniel, Savarese, Fabio, Hofmann, Marco H, Trapani, Francesca, Gmachl, Michael, Botesteanu, Dana-Adriana, Ramharter, Jürgen, Arnhof, Heribert, Schweifer, Norbert, McConnell, Darryl B, Kraut, Norbert
Published in Molecular cancer therapeutics (01.12.2019)
Published in Molecular cancer therapeutics (01.12.2019)
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Journal Article
Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor
Savarese, Fabio, Gollner, Andreas, Rudolph, Dorothea, Lipp, Jesse, Popow, Johannes, Hofmann, Marco H., Arnhof, Heribert, Rinnenthal, Jörg, Trapani, Francesca, Gmachl, Michael, Gerlach, Daniel, Broeker, Joachim, Ettmayer, Peter, Mantoulidis, Andreas, Phan, Jason, Smethurst, Christian A., Treu, Matthias, Waterson, Alex G., Lu, Hengyu, Machado, Annette, Daniele, Joseph, Fesik, Stephan W., Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., McConnell, Darryl B., Petronczki, Mark, Kraut, Norbert, Waizenegger, Irene C.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Abstract 3987: Predicting MCL1 inhibitor sensitivity in large cell line panels using a gene expression signature
Wernitznig, Andreas, Rudolph, Dorothea, Samwer, Matthias, Schweifer, Norbert, Trapani, Francesca, Wunberg, Tobias, Arnhof, Heribert, Lee, Teakyu, Sensintaffar, John L., Olejniczak, Edward T., Benes, Cyril H., Fesik, Stephen W., Kraut, Norbert
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan
Gerlach, Daniel, Gmachl, Michael, Ramharter, Juergen, Teh, Jessica, Fu, Szu-Chin, Trapani, Francesca, Kessler, Dirk, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Hofmann, Marco H.
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Journal Article
Abstract 510: Selective and potent CDK8 inhibitors enhance NK cell activity and promote tumor surveillance
Hofmann, Marco H., Mani, Rajeswaran, Engelhardt, Harald, Impagnatiello, Maria A., Carotta, Sebastian, Kerenyi, Marc A., Lorenzo-Herrero, Seila, Boettcher, Jark, Scharn, Dirk, Arnhof, Heribert, Zoephel, Andreas, Schnitzer, Renate, Gerstberger, Thomas, Rajgolikar, Girish, Goswami, Swagata, Vasu, Sumithira, Ettmayer, Peter, Gonzalez, Segundo R., Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Muthusamy, Natarajan, Moll, Juergen
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract C133: Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406
Hofmann, Marco H, Gmachl, Michael, Ramharter, Jürgen, Savarese, Fabio, Sanderson, Michael P, Gerlach, Daniel, Trapani, Francesca, Botesteanu, Dana-Adriana, Kessler, Dirk, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Schnitzer, Renate, Kofink, Christiane, Stadtmueller, Heinz, Wunberg, Tobias, O’Connell, Jonathan C., Mendes, Rachel L, Richard, David, Saldanha, Adrian S, Moll, Juergen, Pearson, Mark, McConnell, Darryl B, Kraut, Norbert
Published in Molecular cancer therapeutics (01.12.2019)
Published in Molecular cancer therapeutics (01.12.2019)
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