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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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
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
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Donated chemical probes for open science
Müller, Susanne, Ackloo, Suzanne, Arrowsmith, Cheryl H, Bauser, Marcus, Baryza, Jeremy L, Blagg, Julian, Böttcher, Jark, Bountra, Chas, Brown, Peter J, Bunnage, Mark E, Carter, Adrian J, Damerell, David, Dötsch, Volker, Drewry, David H, Edwards, Aled M, Edwards, James, Elkins, Jon M, Fischer, Christian, Frye, Stephen V, Gollner, Andreas, Grimshaw, Charles E, IJzerman, Adriaan, Hanke, Thomas, Hartung, Ingo V, Hitchcock, Steve, Howe, Trevor, Hughes, Terry V, Laufer, Stefan, Li, Volkhart Mj, Liras, Spiros, Marsden, Brian D, Matsui, Hisanori, Mathias, John, O'Hagan, Ronan C, Owen, Dafydd R, Pande, Vineet, Rauh, Daniel, Rosenberg, Saul H, Roth, Bryan L, Schneider, Natalie S, Scholten, Cora, Singh Saikatendu, Kumar, Simeonov, Anton, Takizawa, Masayuki, Tse, Chris, Thompson, Paul R, Treiber, Daniel K, Viana, Amélia Yi, Wells, Carrow I, Willson, Timothy M, Zuercher, William J, Knapp, Stefan, Mueller-Fahrnow, Anke
Published in eLife (20.04.2018)
Published in eLife (20.04.2018)
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Synthesis of Indazoles via N–N Bond-Forming Oxidative Cyclization from 2‑Aminomethyl-phenylamines
Schoeggl Toledano, Anna, Bitai, Jacqueline, Covini, David, Karolyi-Oezguer, Jale, Dank, Christian, Berger, Helmut, Gollner, Andreas
Published in Organic letters (16.02.2024)
Published in Organic letters (16.02.2024)
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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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One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp2)–C(sp3) Cross Coupling and Amide Formation for Proteolysis Targeting Chimera Library Synthesis
Arndt, Christine M., Bitai, Jacqueline, Brunner, Jessica, Opatz, Till, Martinelli, Paola, Gollner, Andreas, Sokol, Kevin R., Krumb, Matthias
Published in Journal of medicinal chemistry (28.12.2023)
Published in Journal of medicinal chemistry (28.12.2023)
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Synthesis of MDM2-p53 Inhibitor BI-0282 via a Dipolar Cycloaddition and Late-Stage Davis–Beirut Reaction
Ramharter, Juergen, Kulhanek, Michael, Dettling, Maike, Gmaschitz, Gerhard, Karolyi-Oezguer, Jale, Weinstabl, Harald, Gollner, Andreas
Published in Organic process research & development (19.08.2022)
Published in Organic process research & development (19.08.2022)
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opnMe.com: a digital initiative for sharing tools with the biomedical research community
Gollner, Andreas, Köster, Markus, Nicklin, Paul, Trieselmann, Thomas, Klein, Elliott, Vlach, Jaromir, Heine, Claudia, Grundl, Marc, Ramharter, Jürgen, Wyatt, David, Chaturvedi, Menorca, Ciulli, Alessio, Carter, Katharine C., Müller, Susanne, Bischoff, Daniel, Ettmayer, Peter, Haaksma, Eric, Mack, Jürgen, McConnell, Darryl, Stenkamp, Dirk, Weinstabl, Harald, Zentgraf, Matthias, Wood, Clive R., Montel, Florian
Published in Nature reviews. Drug discovery (01.07.2022)
Published in Nature reviews. Drug discovery (01.07.2022)
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Discovery and Characterization of Brigimadlin, a Novel and Highly Potent MDM2-p53 Antagonist Suitable for Intermittent Dose Schedules
Gollner, Andreas, Rudolph, Dorothea, Weyer-Czernilofsky, Ulrike, Baumgartinger, Rosa, Jung, Peter, Weinstabl, Harald, Ramharter, Jürgen, Grempler, Rolf, Quant, Jens, Rinnenthal, Jörg, Pérez Pitarch, Alejandro, Golubovic, Bojana, Gerlach, Daniel, Bader, Gerd, Wetzel, Kristiane, Otto, Sebastian, Mandl, Christian, Boehmelt, Guido, McConnell, Darryl B, Kraut, Norbert, Sini, Patrizia
Published in Molecular cancer therapeutics (03.12.2024)
Published in Molecular cancer therapeutics (03.12.2024)
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KRAS Binders Hidden in Nature
Bergner, Andreas, Cockcroft, Xiaoling, Fischer, Gerhard, Gollner, Andreas, Hela, Wolfgang, Kousek, Roland, Mantoulidis, Andreas, Martin, Laetitia J., Mayer, Moriz, Müllauer, Barbara, Siszler, Gabriella, Wolkerstorfer, Bernhard, Kessler, Dirk, McConnell, Darryl B.
Published in Chemistry : a European journal (18.09.2019)
Published in Chemistry : a European journal (18.09.2019)
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Targeting cancer with small-molecule pan-KRAS degraders
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
Published in Science (American Association for the Advancement of Science) (20.09.2024)
Published in Science (American Association for the Advancement of Science) (20.09.2024)
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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor
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
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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Abstract 3197: BI-907828, a novel and potent MDM2-p53 antagonist, acts synergistically in a triple combination with anti-PD-1 and anti-LAG-3 antibodies in syngeneic mouse models of cancer
Rudolph, Dorothea, Weyer-Czernilofsky, Ulrike, Reschke, Markus, Sykora, Martina, Rinnenthal, Jörg, Blake, Sophia, Gremel, Gabriela, Wernitznig, Andreas, Gollner, Andreas, Kraut, Norbert, Moll, Jürgen
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Continuous Flow Synthesis of a Blocked Polyisocyanate: Process Intensification, Reaction Monitoring Via In-Line FTIR Analysis, and Comparative Life Cycle Assessment
Glotz, Gabriel, Waniek, Katharina, Schöggl, Josef-Peter, Cantillo, David, Stueckler, Clemens, Arzt, Anton, Gollner, Andreas, Schipfer, Rudolf, Baumgartner, Rupert J, Kappe, C. Oliver
Published in Organic process research & development (15.10.2021)
Published in Organic process research & development (15.10.2021)
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Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor
Savarese, Fabio, Gollner, Andreas, Rudolph, Dorothea, Lipp, Jesse, Popow, Johannes, Hofmann, Marco H., Arnhof, Heribert, Rinnenthal, Jörg, Trapani, Francesca, Gmachl, Michael, Gerlach, Daniel, Broeker, Joachim, Ettmayer, Peter, Mantoulidis, Andreas, Phan, Jason, Smethurst, Christian A., Treu, Matthias, Waterson, Alex G., Lu, Hengyu, Machado, Annette, Daniele, Joseph, Fesik, Stephan W., Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., McConnell, Darryl B., Petronczki, Mark, Kraut, Norbert, Waizenegger, Irene C.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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