BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design
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
Published in Nature chemical biology (01.07.2019)
Published in Nature chemical biology (01.07.2019)
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Target binding properties and cellular activity of afatinib (BIBW 2992), an irreversible ErbB family blocker
Solca, Flavio, Dahl, Goeran, Zoephel, Andreas, Bader, Gerd, Sanderson, Michael, Klein, Christian, Kraemer, Oliver, Himmelsbach, Frank, Haaksma, Eric, Adolf, Guenther R
Published in The Journal of pharmacology and experimental therapeutics (01.11.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2012)
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Drugging an undruggable pocket on KRAS
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.
Published in Proceedings of the National Academy of Sciences - PNAS (06.08.2019)
Published in Proceedings of the National Academy of Sciences - PNAS (06.08.2019)
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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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Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor
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
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6
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
Published in Cell reports (Cambridge) (19.09.2017)
Published in Cell reports (Cambridge) (19.09.2017)
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Expansion of DUB functionality generated by alternative isoforms - USP35, a case study
Leznicki, Pawel, Natarajan, Jayaprakash, Bader, Gerd, Spevak, Walter, Schlattl, Andreas, Abdul Rehman, Syed Arif, Pathak, Deepika, Weidlich, Simone, Zoephel, Andreas, Bordone, Marie C, Barbosa-Morais, Nuno L, Boehmelt, Guido, Kulathu, Yogesh
Published in Journal of cell science (15.05.2018)
Published in Journal of cell science (15.05.2018)
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Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype
Hirt, Ulrich A., Waizenegger, Irene C., Schweifer, Norbert, Haslinger, Christian, Gerlach, Daniel, Braunger, Jürgen, Weyer-Czernilofsky, Ulrike, Stadtmüller, Heinz, Sapountzis, Ioannis, Bader, Gerd, Zoephel, Andreas, Bister, Bojan, Baum, Anke, Quant, Jens, Kraut, Norbert, Garin-Chesa, Pilar, Adolf, Günther R.
Published in Oncogenesis (New York, NY) (23.02.2018)
Published in Oncogenesis (New York, NY) (23.02.2018)
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N-myc oncogene overexpression down-regulates IL-6; evidence that IL-6 inhibits angiogenesis and suppresses neuroblastoma tumor growth
HATZI, Elissavet, MURPHY, Carol, ZICHE, Marina, ROFSTAD, Einar K, SCHWEIGERER, Lothar, FOTSIS, Theodore, ZOEPHEL, Andreas, RASMUSSEN, Heidi, MORBIDELLI, Lucia, AHORN, Horst, KUNISADA, Keita, TONTSCH, Ulrike, KLENK, Michael, YAMAUCHI-TAKIHARA, Keiko
Published in Oncogene (16.05.2002)
Published in Oncogene (16.05.2002)
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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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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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BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy
Hilberg, Frank, Roth, Gerald J, Krssak, Martin, Kautschitsch, Susanna, Sommergruber, Wolfgang, Tontsch-Grunt, Ulrike, Garin-Chesa, Pilar, Bader, Gerd, Zoephel, Andreas, Quant, Jens, Heckel, Armin, Rettig, Wolfgang J
Published in Cancer research (Chicago, Ill.) (15.06.2008)
Published in Cancer research (Chicago, Ill.) (15.06.2008)
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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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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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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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Crystal Structure of Bisphosphorylated IGF-1 Receptor Kinase
Pautsch, Alexander, Zoephel, Andreas, Ahorn, Horst, Spevak, Walter, Hauptmann, Rudolf, Nar, Herbert
Published in Structure (London) (01.10.2001)
Published in Structure (London) (01.10.2001)
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REPLY TO TRAN ET AL: Dimeric KRAS protein–protein interaction stabilizers
Kessler, Dirk, Gollner, Andreas, Gmachl, Michael, Mantoulidis, Andreas, Martin, Laetitia J., Zoephel, Andreas, Mayer, Moriz, 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.
Published in Proceedings of the National Academy of Sciences - PNAS (18.02.2020)
Published in Proceedings of the National Academy of Sciences - PNAS (18.02.2020)
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Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Sini, Patrizia, Gürtler, Ulrich, Zahn, Stephan K, Baumann, Christoph, Rudolph, Dorothea, Baumgartinger, Rosa, Strauss, Eva, Haslinger, Christian, Tontsch-Grunt, Ulrike, Waizenegger, Irene C, Solca, Flavio, Bader, Gerd, Zoephel, Andreas, Treu, Matthias, Reiser, Ulrich, Garin-Chesa, Pilar, Boehmelt, Guido, Kraut, Norbert, Quant, Jens, Adolf, Günther R
Published in Molecular cancer therapeutics (01.10.2016)
Published in Molecular cancer therapeutics (01.10.2016)
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