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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In Vitro and In Vivo Activities of the Novel Anticytomegalovirus Compound AIC246
Lischka, Peter, Hewlett, Guy, Wunberg, Tobias, Baumeister, Judith, Paulsen, Daniela, Goldner, Thomas, Ruebsamen-Schaeff, Helga, Zimmermann, Holger
Published in Antimicrobial Agents and Chemotherapy (01.03.2010)
Published in Antimicrobial Agents and Chemotherapy (01.03.2010)
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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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Catalytic asymmetric hydrogenation of heterocyclic ketone-derived hydrazones, pronounced solvent effect on the inversion of configuration
Haddad, Nizar, Qu, Bo, Rodriguez, Sonia, van der Veen, Lars, Reeves, Diana C., Gonnella, Nina C., Lee, Heewon, Grinberg, Nelu, Ma, Shengli, Krishnamurthy, Dhileepkumar, Wunberg, Tobias, Senanayake, Chris H.
Published in Tetrahedron letters (20.07.2011)
Published in Tetrahedron letters (20.07.2011)
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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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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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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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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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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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Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1
Böttcher, Jark, Fuchs, Julian E., Mayer, Moriz, Kahmann, Jan, Zak, Krzysztof M., Wunberg, Tobias, Woehrle, Simon, Kessler, Dirk
Published in Archiv der Pharmazie (Weinheim) (01.06.2024)
Published in Archiv der Pharmazie (Weinheim) (01.06.2024)
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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 (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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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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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 PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors
Hofmann, Marco H, Gmachl, Michael, Ramharter, Jürgen, Savarese, Fabio, Gerlach, Daniel, Marszalek, Joseph R, Sanderson, Michael P, Trapani, Francesca, Kessler, Dirk, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Fu, Szu-Chin, Teh, Jessica, Vellano, Christopher P., O’Connell, Jonathan C., Mendes, Rachel L, Moll, Juergen, Heffernan, Timothy P., 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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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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Journal Article
Abstract B103: Development and characterisation of KRASmulti inhibitors for the treatment of KRAS mutant pancreatic ductal adenocarcinoma
Tedeschi, Antonio, Schaaf, Otmar, Gmachl, Michael, Herdeis, Lorenz, Rocchetti, Francesca, Popow, Johannes, Schischlik, Fiorella, Gerlach, Daniel, Lipp, Jesse, Bröker, Joachim, Mantoulidis, Andreas, Smethurst, Chris, Kessler, Dirk, Boettcher, Jark, Wunberg, Tobias, Santoro, Valeria, Waterson, Alex, Phan, Jason, Little, Andrew, Abbott, Jason, Sun, Qi, Fesik, Stephen, Mcconnell, Darryl, Pearson, Mark A., Kraut, Norbert, Rudolph, Dorothea
Published in Cancer research (Chicago, Ill.) (16.01.2024)
Published in Cancer research (Chicago, Ill.) (16.01.2024)
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암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체
GOLLNER ANDREAS, STADTMUELLER HEINZ, TREU MATTHIAS, LITTLE ANDREW, MANTOULIDIS ANDREAS, CUI JIANWEN, HODGES TIM, PHAN JASON, HERDEIS LORENZ, SMETHURST CHRISTIAN ALAN PAUL, WUNBERG TOBIAS, SARKAR DHRUBA, SOKOL KEVIN, WILDING BIRGIT, FUCHS JULIAN, WATERSON ALEX, FESIK STEPHEN W, BROEKER JOACHIM, RAMHARTER JUERGEN, ABBOTT JASON, SUN QI
Year of Publication 27.08.2024
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Year of Publication 27.08.2024
Patent
Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens
Schischlik, Fiorella, Tedeschi, Antonio, Rudolph, Dorothea, Gerlach, Daniel, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Herdeis, Lorenz, Broeker, Joachim, Wunberg, Tobias, Boghossian, Andrew S., Rees, Matthew G., Ronan, Melissa M., Roth, Jennifer A., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Haslinger, Christian, Lipp, Jesse
Published in Molecular cancer therapeutics (01.12.2023)
Published in Molecular cancer therapeutics (01.12.2023)
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Journal Article
Abstract A087: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models
Peng, David H, Tedeschi, Antonio, Herdeis, Lorenz, Savarese, Fabio, Rocchetti, Francesca, Johannes, Popow, Huber, Heinrich J, Melillo, Nicola, Dickinson, Jake, Mistry, Hitesh B, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Broker, Joachim, Wunberg, Tobias, Schischlik, Fiorella, Lipp, Jesse, Ramamoorthy, Vandhana, Daniele, Joseph R, Kopetz, Scott, Kim, Michael, Gibbons, Don L, Vellano, Christopher P, Marszalek, Joseph R, Heffernan, Timothy P, McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Molecular cancer therapeutics (01.12.2023)
Published in Molecular cancer therapeutics (01.12.2023)
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