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

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A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo von Kofink, Christiane, Trainor, Nicole, Mair, Barbara, Wöhrle, Simon, Wurm, Melanie, Mischerikow, Nikolai, Roy, Michael J., Bader, Gerd, Greb, Peter, Garavel, Géraldine, Diers, Emelyne, McLennan, Ross, Whitworth, Claire, Vetma, Vesna, Rumpel, Klaus, Scharnweber, Maximilian, Fuchs, Julian E., Gerstberger, Thomas, Cui, Yunhai, Gremel, Gabriela, Chetta, Paolo, Hopf, Stefan, Budano, Nicole, Rinnenthal, Joerg, Gmaschitz, Gerhard, Mayer, Moriz, Koegl, Manfred, Ciulli, Alessio, Weinstabl, Harald, Farnaby, William

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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 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

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Synthesis of Functionalized Diarylmethanes via a Copper-Catalyzed Cross-Coupling of Arylmagnesium Reagents with Benzylic Phosphates von Kofink, Christiane C, Knochel, Paul

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Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria von Junk, Lukas, Schmiedel, Volker M., Guha, Somraj, Fischel, Katharina, Greb, Peter, Vill, Kristin, Krisilia, Violetta, van Geelen, Lasse, Rumpel, Klaus, Kaur, Parvinder, Krishnamurthy, Ramya V., Narayanan, Shridhar, Shandil, Radha Krishan, Singh, Mayas, Kofink, Christiane, Mantoulidis, Andreas, Biber, Philipp, Gmaschitz, Gerhard, Kazmaier, Uli, Meinhart, Anton, Leodolter, Julia, Hoi, David, Junker, Sabryna, Morreale, Francesca Ester, Clausen, Tim, Kalscheuer, Rainer, Weinstabl, Harald, Boehmelt, Guido

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Asymmetric Construction of Rings A−D of Daphnicyclidin-Type Alkaloids von Dunn, Travis B, Ellis, J. Michael, Kofink, Christiane C, Manning, James R, Overman, Larry E

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Iron-Catalyzed Aryl-Aryl Cross-Couplings with Magnesium-Derived Copper Reagents von Sapountzis, Ioannis, Lin, Wenwei, Kofink, Christiane C., Despotopoulou, Christina, Knochel, Paul

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Iron-catalyzed aryl-aryl cross-coupling reaction tolerating amides and unprotected quinolinones von Kofink, Christiane C, Blank, Benoit, Pagano, Sandro, Götz, Nadine, Knochel, Paul

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Preparation of Aryl−Alkylamines via Electrophilic Amination of Functionalized Arylazo Tosylates with Alkylzinc Reagents von Sinha, Pradipta, Kofink, Christiane C, Knochel, Paul

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Efficient Cross-Coupling of Functionalized Arylzinc Halides Catalyzed by a Nickel Chloride−Diethyl Phosphite System von Gavryushin, Andrei, Kofink, Christiane, Manolikakes, Georg, Knochel, Paul

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Electrochemical Rearrangement of 3‑Hydroxyoxindoles into Benzoxazinones von Vayer, Marie, Pastor, Miryam, Kofink, Christiane, Maulide, Nuno

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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

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Targeting cancer with small-molecule pan-KRAS degraders von 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

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Confounding Factors in Targeted Degradation of Short-Lived Proteins von Vetma, Vesna, Perez, Laura Casares, Eliaš, Ján, Stingu, Andrea, Kombara, Anju, Gmaschitz, Teresa, Braun, Nina, Ciftci, Tuncay, Dahmann, Georg, Diers, Emelyne, Gerstberger, Thomas, Greb, Peter, Kidd, Giorgia, Kofink, Christiane, Puoti, Ilaria, Spiteri, Valentina, Trainor, Nicole, Weinstabl, Harald, Westermaier, Yvonne, Whitworth, Claire, Ciulli, Alessio, Farnaby, William, McAulay, Kirsten, Frost, Aileen B., Chessum, Nicola, Koegl, Manfred

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A Chiral Pool Strategy for the Synthesis of a SMARCA2 Degrading PROTAC von Lee, Miseon, Wu, Jiang-Ping, Lee, Jaehee, Wang, Jun, White, Jada A. H., Rugg, Kyle W., Sienkiewicz, Alexander, Lorenz, Jon C., Greb, Peter, Bunner, Matthew H., Hirsh, David A., Gonnella, Nina C., Nordstrom, Fredrik L., Kofink, Christiane, Weinstabl, Harald, Reeves, Jonathan T.

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Getting a Grip on the Undrugged: Targeting β‐Catenin with Fragment‐Based Methods von Kessler, Dirk, Mayer, Moriz, Zahn, Stephan K., Zeeb, Markus, Wöhrle, Simon, Bergner, Andreas, Bruchhaus, Jens, Ciftci, Tuncay, Dahmann, Georg, Dettling, Maike, Döbel, Sandra, Fuchs, Julian E., Geist, Leonhard, Hela, Wolfgang, Kofink, Christiane, Kousek, Roland, Moser, Franziska, Puchner, Teresa, Rumpel, Klaus, Scharnweber, Maximilian, Werni, Patrick, Wolkerstorfer, Bernhard, Breitsprecher, Dennis, Baaske, Philipp, Pearson, Mark, McConnell, Darryl B., Böttcher, Jark

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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.

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An efficient Negishi cross-coupling reaction catalyzed by nickel(II) and diethyl phosphite von Gavryushin, Andrei, Kofink, Christiane, Manolikakes, Georg, Knochel, Paul

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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

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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

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