Drugging an undruggable pocket on KRAS von Kesslera, Dirk, Gmachla, Michael, Mantoulidisa, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, Gollner, Andreas, Covini, David, Fischer, Silke, Gerstberger, Thomas, Gmaschitz, Teresa, Goodwin, Craig, Greb, Peter, Häring, Daniela, Hela, Wolfgang, Hoffmann, Johann, Karolyi-Oezguer, Jale, Knesl, Petr, Kornigg, Stefan, Koegl, Manfred, Kousek, Roland, Lamarre, Lyne, Moser, Franziska, Munico-Martinez, Silvia, Peinsipp, Christoph, Phan, Jason, Rinnenthal, Jörg, Sai, Jiqing, Salamon, Christian, Scherbantin, Yvonne, Schipany, Katharina, Schnitzer, Renate, Schrenk, Andreas, Sharps, Bernadette, Siszler, Gabriella, Sun, Qi, Waterson, Alex, Wolkerstorfer, Bernhard, Zeeb, Markus, Pearson, Mark, Fesik, Stephen W., McConnell, Darryl B.

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BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design von 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

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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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Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor von Martin, Laetitia J, Koegl, Manfred, Bader, Gerd, Cockcroft, Xiao-Ling, Fedorov, Oleg, Fiegen, Dennis, Gerstberger, Thomas, Hofmann, Marco H, Hohmann, Anja F, Kessler, Dirk, Knapp, Stefan, Knesl, Petr, Kornigg, Stefan, Müller, Susanne, Nar, Herbert, Rogers, Catherine, Rumpel, Klaus, Schaaf, Otmar, Steurer, Steffen, Tallant, Cynthia, Vakoc, Christopher R, Zeeb, Markus, Zoephel, Andreas, Pearson, Mark, Boehmelt, Guido, McConnell, Darryl

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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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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

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Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6 von Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Berger, Helmut, Caligiuri, Maureen, Dank, Christian, Engen, John R., Ettmayer, Peter, Fischerauer, Bernhard, Flotzinger, Gerlinde, Gerlach, Daniel, Gerstberger, Thomas, Gmaschitz, Teresa, Greb, Peter, Han, Bingsong, Heyes, Elizabeth, Iacob, Roxana E., Kessler, Dirk, Kölle, Heike, Lamarre, Lyne, Lancia, David R., Lucas, Simon, Mayer, Moriz, Mayr, Katharina, Mischerikow, Nikolai, Mück, Katja, Peinsipp, Christoph, Petermann, Oliver, Reiser, Ulrich, Rudolph, Dorothea, Rumpel, Klaus, Salomon, Carina, Scharn, Dirk, Schnitzer, Renate, Schrenk, Andreas, Schweifer, Norbert, Thompson, Diane, Traxler, Elisabeth, Varecka, Roland, Voss, Tilman, Weiss-Puxbaum, Alexander, Winkler, Sandra, Zheng, Xiaozhang, Zoephel, Andreas, Kraut, Norbert, McConnell, Darryl, Pearson, Mark, Koegl, Manfred

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Unconventional tethering of Ulp1 to the transport channel of the nuclear pore complex by karyopherins von Panse, Vikram Govind, Küster, Bernhard, Gerstberger, Thomas, Hurt, Ed

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The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML von Gerlach, Daniel, Tontsch-Grunt, Ulrike, Baum, Anke, Popow, Johannes, Scharn, Dirk, Hofmann, Marco H., Engelhardt, Harald, Kaya, Onur, Beck, Janina, Schweifer, Norbert, Gerstberger, Thomas, Zuber, Johannes, Savarese, Fabio, Kraut, Norbert

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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

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Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition von Hohmann, Anja F, Martin, Laetitia J, Minder, Jessica L, Roe, Jae-Seok, Shi, Junwei, Steurer, Steffen, Bader, Gerd, McConnell, Darryl, Pearson, Mark, Gerstberger, Thomas, Gottschamel, Teresa, Thompson, Diane, Suzuki, Yutaka, Koegl, Manfred, Vakoc, Christopher R

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Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis von 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

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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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Chasing Red Herrings: Palladium Metal Salt Impurities Feigning KRAS Activity in Biochemical Assays von Gerstberger, Thomas, Berger, Helmut, Büttner, Frank H., Gmachl, Michael, Kessler, Dirk, Koegl, Manfred, Lucas, Simon, Martin, Laetitia J., Mayer, Moriz, McConnell, Darryl B., Mitzner, Sophie, Scholz, Guido, Treu, Matthias, Wolkerstorfer, Bernhard, Zahn, Stephan, Zak, Krzysztof M., Jaeger, Philipp A., Ettmayer, Peter

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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.

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Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance von 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

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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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Yeast Ran-Binding Protein 1 (Yrb1) Shuttles between the Nucleus and Cytoplasm and Is Exported from the Nucleus via a CRM1(XPO1)-Dependent Pathway von Künzler, Markus, Gerstberger, Thomas, Stutz, Françoise, Bischoff, F. Ralf, Hurt, Ed

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Abstract 1472: Novel EGFR WT sparing, HER2 selective inhibitors for the treatment of HER2 exon 20 insertion driven tumors address a clear unmet medical need von Neumüller, Ralph A., Wilding, Birgit, Scharn, Dirk, Böse, Dietrich, Santoro, Valeria, Gerlach, Daniel, Ettmayer, Peter, Gerstberger, Thomas, Fuchs, Julian, Treu, Matthias, Zahn, Stephan, Baum, Anke, Chetta, Paolo, Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Solca, Flavio

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