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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Journal Article
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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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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Journal Article
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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Journal Article
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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Journal Article
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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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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Journal Article
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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Journal Article
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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Journal Article
Abstract 510: Selective and potent CDK8 inhibitors enhance NK cell activity and promote tumor surveillance
Hofmann, Marco H., Mani, Rajeswaran, Engelhardt, Harald, Impagnatiello, Maria A., Carotta, Sebastian, Kerenyi, Marc A., Lorenzo-Herrero, Seila, Boettcher, Jark, Scharn, Dirk, Arnhof, Heribert, Zoephel, Andreas, Schnitzer, Renate, Gerstberger, Thomas, Rajgolikar, Girish, Goswami, Swagata, Vasu, Sumithira, Ettmayer, Peter, Gonzalez, Segundo R., Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Muthusamy, Natarajan, Moll, Juergen
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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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 4630: Development of selective and potent CDK8 inhibitors that increase NK cell activity, which translates in tumor surveillance
Hofmann, Marco H., Engelhardt, Harald, Carotta, Sebastian, Arnhof, Heribert, Scharn, Dirk, Kerenyi, Marc, Mayer, Moritz, Gmaschitz, Gerhard, Egger, Georg, Engelhardt, Christian, Sanderson, Michael, Impagnatiello, Maria A., Schnitzer, Renate, Pearson, Mark, McConnell, Darryl, Kraut, Norbert, Moll, Jürgen
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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Journal Article
Abstract 3354: Chemically induced degradation of the transcription factor BCL6
Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Caligiuri, Maureen, Dank, Christian, Engen, John R., Ettmayer, Peter, Gerlach, Daniel, Gerstberger, Thomas, Han, Bingsong, Iacob, Roxana E., Kessler, Dirk, Lancia, David R., Moriz, Mayer, Mischerikow, Nikolai, Rumpel, Klaus, Schnitzer, Renate, Voss, Tilman, Zheng, Xiaozhang, Zoephel, Andreas, Kraut, Norbert, McConnell, Darryl, Pearson, Mark, Koegl, Manfred
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Publisher Correction: 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 (01.08.2019)
Published in Nature chemical biology (01.08.2019)
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Abstract 1525: Chemically induced degradation of the oncogenic transcription factor BCL6
Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Berger, Helmut, Blake, Sophia, Caligiuri, Maureen, Engen, John, Ettmayer, Peter, Gerstberger, Thomas, Gerlach, Daniel, Jacob, Roxana, Lucas, Simon, Mayer, Moriz, Nikolai, Mischerikow, Klaus, Rumpel, Dirk, Scharn, Renate, Schnitzer, Voss, Tilman, Andreas, Zoephel, Kraut, Norbert, McConnell, Darryl, Mark, Pearson, Koegl, Manfred
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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A comparative cell-based high throughput screening strategy for the discovery of selective tyrosine kinase inhibitors with anticancer activity
Stratowa, C, Baum, A, Castañon, M J, Dahmann, G, Himmelsbach, F, Himmler, A, Loeber, G, Metz, T, Schnitzer, R, Solca, F, Spevak, W, Tontsch, U, von Rüden, T
Published in Anti-cancer drug design (01.10.1999)
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Published in Anti-cancer drug design (01.10.1999)
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PROCEDIMENTO PARA O RASTERIO COMPARATIVO DE SUBSTANCIAS FARMACOLOGICAMENTE ACTIVAS
WALTER SPEVAK, ADOLF HIMMLER, MARIA JOSEFA WICHE-CASTANON, ULRIKE TONTSCH, GERHARD LOEBER, RENATE SCHNITZER, ARMIN PETER CZERNILOFSKY, CHRISTIAN STRATOWA, ULRIKE WEYER-CZERNILOFSKY, THOMAS VON RUDEN, THOMAS METZ
Year of Publication 30.01.2004
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Year of Publication 30.01.2004
Patent
Fremgangsmåde til sammenlignende gennemsøgning af stoffer med farmakologisk virkning
WEYER-CZERNILOFSKY, ULRIKE, LOEBER, GERHARD, VON RUEDEN, THOMAS, TONTSCH, ULRIKE, SCHNITZER, RENATE, WICHE-CASTANON, MARIA, JOSEFA, CZERNILOFSKY, ARMIN, PETER, METZ, THOMAS, STRATOWA, CHRISTIAN, HIMMLER, ADOLF, SPEVAK, WALTER
Year of Publication 01.12.2003
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Year of Publication 01.12.2003
Patent
VERFAHREN ZUM VERGLEICHENDEN SCREENEN VON SUBSTANZEN MIT PHARMAKOLOGISCHER WIRKUNG
WEYER-CZERNILOFSKY, ULRIKE, LOEBER, GERHARD, VON RUEDEN, THOMAS, TONTSCH, ULRIKE, SCHNITZER, RENATE, WICHE-CASTANON, MARIA, JOSEFA, CZERNILOFSKY, ARMIN, PETER, METZ, THOMAS, STRATOWA, CHRISTIAN, HIMMLER, ADOLF, SPEVAK, WALTER
Year of Publication 15.09.2003
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Year of Publication 15.09.2003
Patent