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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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)
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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)
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Journal Article
Tumor cell‐specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase
Peter, Stefanie, Bultinck, Jennyfer, Myant, Kevin, Jaenicke, Laura A, Walz, Susanne, Müller, Judith, Gmachl, Michael, Treu, Matthias, Boehmelt, Guido, Ade, Carsten P, Schmitz, Werner, Wiegering, Armin, Otto, Christoph, Popov, Nikita, Sansom, Owen, Kraut, Norbert, Eilers, Martin
Published in EMBO molecular medicine (01.12.2014)
Published in EMBO molecular medicine (01.12.2014)
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Journal Article
The RING-H2 Finger Protein APC11 and the E2 Enzyme UBC4 Are Sufficient to Ubiquitinate Substrates of the Anaphase-Promoting Complex
Gmachl, Michael, Gieffers, Christian, Podtelejnikov, Alexandre V., Mann, Matthias, Peters, Jan-Michael
Published in Proceedings of the National Academy of Sciences - PNAS (01.08.2000)
Published in Proceedings of the National Academy of Sciences - PNAS (01.08.2000)
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Journal Article
A possible docking and fusion particle for synaptic transmission
Schiavo, Giampietro, Gmachl, Michael J. S, Stenbeck, Gudrun, Söllner, Thomas H, Rothman, James E
Published in Nature (London) (14.12.1995)
Published in Nature (London) (14.12.1995)
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Anterograde Flow of Cargo across the Golgi Stack Potentially Mediated via Bidirectional "Percolating" COPI Vesicles
Orci, Lelio, Ravazzola, Mariella, Volchuk, Allen, Engel, Thomas, Gmachl, Michael, Amherdt, Mylene, Perrelet, Alain, Sollner, Thomas H., Rothman, James E.
Published in Proceedings of the National Academy of Sciences - PNAS (12.09.2000)
Published in Proceedings of the National Academy of Sciences - PNAS (12.09.2000)
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Journal Article
KRAS Secondary Mutations That Confer Acquired Resistance to KRAS G12C Inhibitors, Sotorasib and Adagrasib, and Overcoming Strategies: Insights From In Vitro Experiments
Koga, Takamasa, Suda, Kenichi, Fujino, Toshio, Ohara, Shuta, Hamada, Akira, Nishino, Masaya, Chiba, Masato, Shimoji, Masaki, Takemoto, Toshiki, Arita, Takeo, Gmachl, Michael, Hofmann, Marco H., Soh, Junichi, Mitsudomi, Tetsuya
Published in Journal of thoracic oncology (01.08.2021)
Published in Journal of thoracic oncology (01.08.2021)
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Journal Article
The human sperm protein PH-20 has hyaluronidase activity
Gmachl, Michael, Sagan, Sandrine, Ketter, Sigrid, Kreil, Günther
Published in FEBS letters (28.12.1993)
Published in FEBS letters (28.12.1993)
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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
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)
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Journal Article
Abstract CT210: Trial in Process: Phase 1 studies of BI 1701963, a SOS1::KRAS Inhibitor, in combination with MEK inhibitors, irreversible KRASG12C inhibitors or irinotecan
Hofmann, Marco H., Lu, Hengyu, Duenzinger, Ulrich, Gerlach, Daniel, Trapani, Francesca, Machado, Annette A., Daniele, Joseph R., Waizenegger, Irene, Gmachl, Michael, Rudolph, Dorothea, Vellano, Christopher P., Marotti, Marcelo, Vucenovic, Vitomir, Heffernan, Timothy P., Marszalek, Joseph R., Petronczki, Mark P., Kraut, Norbert
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Journal Article
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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Journal Article
Abstract A030: Evaluation of phosphoprotein- and transcript-based pharmacodynamic biomarkers in pre-clinical studies of the novel SOS1::KRAS inhibitor BI-3406
Gerlach, Daniel, Savarese, Fabio, Hofmann, Marco H, Trapani, Francesca, Gmachl, Michael, Botesteanu, Dana-Adriana, Ramharter, Jürgen, Arnhof, Heribert, Schweifer, Norbert, 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 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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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 1091: BI-3406 and BI 1701963: Potent and selective SOS1::KRAS inhibitors induce regressions in combination with MEK inhibitors or irinotecan
Gerlach, Daniel, Gmachl, Michael, Ramharter, Juergen, Teh, Jessica, Fu, Szu-Chin, Trapani, Francesca, Kessler, Dirk, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Hofmann, Marco H.
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Journal Article
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 PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors
Hofmann, Marco H, Gmachl, Michael, Ramharter, Jürgen, Savarese, Fabio, Gerlach, Daniel, Marszalek, Joseph R, Sanderson, Michael P, Trapani, Francesca, Kessler, Dirk, Rumpel, Klaus, Botesteanu, Dana-Adriana, Ettmayer, Peter, Arnhof, Heribert, Gerstberger, Thomas, Kofink, Christiane, Wunberg, Tobias, Fu, Szu-Chin, Teh, Jessica, Vellano, Christopher P., O’Connell, Jonathan C., Mendes, Rachel L, Moll, Juergen, Heffernan, Timothy P., 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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