BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition von 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

Volltext

In Vitro and In Vivo Activities of the Novel Anticytomegalovirus Compound AIC246 von Lischka, Peter, Hewlett, Guy, Wunberg, Tobias, Baumeister, Judith, Paulsen, Daniela, Goldner, Thomas, Ruebsamen-Schaeff, Helga, Zimmermann, Holger

Volltext

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 von 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

Volltext

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor von 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

Volltext

Catalytic asymmetric hydrogenation of heterocyclic ketone-derived hydrazones, pronounced solvent effect on the inversion of configuration von 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.

Volltext

Pan-KRAS inhibitor disables oncogenic signalling and tumour growth von 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

Volltext

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors von 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

Volltext

One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS von 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

Volltext

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3 von 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.

Volltext

Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1 von Böttcher, Jark, Fuchs, Julian E., Mayer, Moriz, Kahmann, Jan, Zak, Krzysztof M., Wunberg, Tobias, Woehrle, Simon, Kessler, Dirk

Volltext

Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors von 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.

Volltext

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor von 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

Volltext

Abstract 3987: Predicting MCL1 inhibitor sensitivity in large cell line panels using a gene expression signature von 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

Volltext

Abstract 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan von 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.

Volltext

Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors von 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

Volltext

Abstract C133: Effective targeting of KRAS-driven tumors by the first-in-class, orally bioavailable SOS1::KRAS inhibitor BI-3406 von 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

Volltext

Improving the hit-to-lead process: data-driven assessment of drug-like and lead-like screening hits von Wunberg, Tobias, Hendrix, Martin, Hillisch, Alexander, Lobell, Mario, Meier, Heinrich, Schmeck, Carsten, Wild, Hanno, Hinzen, Berthold

Volltext

Abstract A085: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validat... von Tedeschi, Antonio, Herdeis, Lorenz, Santoro, Valeria, Savarese, Fabio, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Bröker, Joachim, Wunberg, Tobias, Gmachl, Michael, Klaus, Rumpel, Schischlik, Fiorella, Lipp, Jesse, Peng, David H., Williams, Mariah, Deckard, Charles, Ramamoorthy, Vandhana, Daniele, Joseph R., Ajani, Jaffer A., Meric-Bernstam, Funda, Vellano, Christopher P., Marszalek, Joseph R., Heffernan, Timothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea

Volltext

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 m... von 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

Volltext

Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens von 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

Volltext