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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
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)
Get full text
Journal Article
Native Mass Spectrometry Can Effectively Predict PROTAC Efficacy
Beveridge, Rebecca, Kessler, Dirk, Rumpel, Klaus, Ettmayer, Peter, Meinhart, Anton, Clausen, Tim
Published in ACS central science (22.07.2020)
Published in ACS central science (22.07.2020)
Get full text
Journal Article
HUWE1 employs a giant substrate-binding ring to feed and regulate its HECT E3 domain
Grabarczyk, Daniel B., Petrova, Olga A., Deszcz, Luiza, Kurzbauer, Robert, Murphy, Paul, Ahel, Juraj, Vogel, Antonia, Gogova, Rebeca, Faas, Victoria, Kordic, Darja, Schleiffer, Alexander, Meinhart, Anton, Imre, Richard, Lehner, Anita, Neuhold, Jana, Bader, Gerd, Stolt-Bergner, Peggy, Böttcher, Jark, Wolkerstorfer, Bernhard, Fischer, Gerhard, Grishkovskaya, Irina, Haselbach, David, Kessler, Dirk, Clausen, Tim
Published in Nature chemical biology (01.10.2021)
Published in Nature chemical biology (01.10.2021)
Get full text
Journal Article
Direct NMR Probing of Hydration Shells of Protein Ligand Interfaces and Its Application to Drug Design
Geist, Leonhard, Mayer, Moriz, Cockcroft, Xiao-Ling, Wolkerstorfer, Bernhard, Kessler, Dirk, Engelhardt, Harald, McConnell, Darryl B, Konrat, Robert
Published in Journal of medicinal chemistry (09.11.2017)
Published in Journal of medicinal chemistry (09.11.2017)
Get full text
Journal Article
A ligand discovery toolbox for the WWE domain family of human E3 ligases
Münzker, Lena, Kimani, Serah W., Fowkes, Milan M., Dong, Aiping, Zheng, Hong, Li, Yanjun, Dasovich, Morgan, Zak, Krzysztof M., Leung, Anthony K. L., Elkins, Jonathan M., Kessler, Dirk, Arrowsmith, Cheryl H., Halabelian, Levon, Böttcher, Jark
Published in Communications biology (24.07.2024)
Published in Communications biology (24.07.2024)
Get full text
Journal Article
Targeting Son of Sevenless 1: The pacemaker of KRAS
Kessler, Dirk, Gerlach, Daniel, Kraut, Norbert, McConnell, Darryl B.
Published in Current opinion in chemical biology (01.06.2021)
Published in Current opinion in chemical biology (01.06.2021)
Get full text
Journal Article
Stopping the beating heart of cancer: KRAS reviewed
Herdeis, Lorenz, Gerlach, Daniel, McConnell, Darryl B., Kessler, Dirk
Published in Current opinion in structural biology (01.12.2021)
Published in Current opinion in structural biology (01.12.2021)
Get full text
Journal Article
The hanging heart: How KRAS lures its prey to the membrane
Kessler, Dirk, McConnell, Darryl B.
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2020)
Published in Proceedings of the National Academy of Sciences - PNAS (27.10.2020)
Get full text
Journal Article
PI by NMR: Probing CH–π Interactions in Protein–Ligand Complexes by NMR Spectroscopy
Platzer, Gerald, Mayer, Moriz, Beier, Andreas, Brüschweiler, Sven, Fuchs, Julian E., Engelhardt, Harald, Geist, Leonhard, Bader, Gerd, Schörghuber, Julia, Lichtenecker, Roman, Wolkerstorfer, Bernhard, Kessler, Dirk, McConnell, Darryl B., Konrat, Robert
Published in Angewandte Chemie International Edition (24.08.2020)
Published in Angewandte Chemie International Edition (24.08.2020)
Get full text
Journal Article
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)
Get full text
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)
Get full text
Journal Article
Drugging all RAS isoforms with one pocket
Kessler, Dirk, Bergner, Andreas, Böttcher, Jark, Fischer, Gerhard, Döbel, Sandra, Hinkel, Melanie, Müllauer, Barbara, Weiss-Puxbaum, Alexander, McConnell, Darryl B
Published in Future medicinal chemistry (01.11.2020)
Published in Future medicinal chemistry (01.11.2020)
Get full text
Journal Article
Chasing Red Herrings: Palladium Metal Salt Impurities Feigning KRAS Activity in Biochemical Assays
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
Published in Journal of medicinal chemistry (25.07.2024)
Published in Journal of medicinal chemistry (25.07.2024)
Get full text
Journal Article
Ligandability assessment of the C‐terminal Rel‐homology domain of NFAT1
Böttcher, Jark, Fuchs, Julian E., Mayer, Moriz, Kahmann, Jan, Zak, Krzysztof M., Wunberg, Tobias, Woehrle, Simon, Kessler, Dirk
Published in Archiv der Pharmazie (Weinheim) (01.06.2024)
Published in Archiv der Pharmazie (Weinheim) (01.06.2024)
Get full text
Journal Article
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)
Get full text
Journal Article
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)
Get full text
Journal Article