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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A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Kofink, Christiane, Trainor, Nicole, Mair, Barbara, Wöhrle, Simon, Wurm, Melanie, Mischerikow, Nikolai, Roy, Michael J., Bader, Gerd, Greb, Peter, Garavel, Géraldine, Diers, Emelyne, McLennan, Ross, Whitworth, Claire, Vetma, Vesna, Rumpel, Klaus, Scharnweber, Maximilian, Fuchs, Julian E., Gerstberger, Thomas, Cui, Yunhai, Gremel, Gabriela, Chetta, Paolo, Hopf, Stefan, Budano, Nicole, Rinnenthal, Joerg, Gmaschitz, Gerhard, Mayer, Moriz, Koegl, Manfred, Ciulli, Alessio, Weinstabl, Harald, Farnaby, William
Published in Nature communications (10.10.2022)
Published in Nature communications (10.10.2022)
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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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Homo-BacPROTAC-induced degradation of ClpC1 as a strategy against drug-resistant mycobacteria
Junk, Lukas, Schmiedel, Volker M., Guha, Somraj, Fischel, Katharina, Greb, Peter, Vill, Kristin, Krisilia, Violetta, van Geelen, Lasse, Rumpel, Klaus, Kaur, Parvinder, Krishnamurthy, Ramya V., Narayanan, Shridhar, Shandil, Radha Krishan, Singh, Mayas, Kofink, Christiane, Mantoulidis, Andreas, Biber, Philipp, Gmaschitz, Gerhard, Kazmaier, Uli, Meinhart, Anton, Leodolter, Julia, Hoi, David, Junker, Sabryna, Morreale, Francesca Ester, Clausen, Tim, Kalscheuer, Rainer, Weinstabl, Harald, Boehmelt, Guido
Published in Nature communications (05.03.2024)
Published in Nature communications (05.03.2024)
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Asymmetric Construction of Rings A−D of Daphnicyclidin-Type Alkaloids
Dunn, Travis B, Ellis, J. Michael, Kofink, Christiane C, Manning, James R, Overman, Larry E
Published in Organic letters (17.12.2009)
Published in Organic letters (17.12.2009)
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Electrochemical Rearrangement of 3‑Hydroxyoxindoles into Benzoxazinones
Vayer, Marie, Pastor, Miryam, Kofink, Christiane, Maulide, Nuno
Published in Organic letters (14.01.2022)
Published in Organic letters (14.01.2022)
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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
Confounding Factors in Targeted Degradation of Short-Lived Proteins
Vetma, Vesna, Perez, Laura Casares, Eliaš, Ján, Stingu, Andrea, Kombara, Anju, Gmaschitz, Teresa, Braun, Nina, Ciftci, Tuncay, Dahmann, Georg, Diers, Emelyne, Gerstberger, Thomas, Greb, Peter, Kidd, Giorgia, Kofink, Christiane, Puoti, Ilaria, Spiteri, Valentina, Trainor, Nicole, Weinstabl, Harald, Westermaier, Yvonne, Whitworth, Claire, Ciulli, Alessio, Farnaby, William, McAulay, Kirsten, Frost, Aileen B., Chessum, Nicola, Koegl, Manfred
Published in ACS chemical biology (19.07.2024)
Published in ACS chemical biology (19.07.2024)
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Journal Article
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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A Chiral Pool Strategy for the Synthesis of a SMARCA2 Degrading PROTAC
Lee, Miseon, Wu, Jiang-Ping, Lee, Jaehee, Wang, Jun, White, Jada A. H., Rugg, Kyle W., Sienkiewicz, Alexander, Lorenz, Jon C., Greb, Peter, Bunner, Matthew H., Hirsh, David A., Gonnella, Nina C., Nordstrom, Fredrik L., Kofink, Christiane, Weinstabl, Harald, Reeves, Jonathan T.
Published in Organic process research & development (19.04.2024)
Published in Organic process research & development (19.04.2024)
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Getting a Grip on the Undrugged: Targeting β‐Catenin with Fragment‐Based Methods
Kessler, Dirk, Mayer, Moriz, Zahn, Stephan K., Zeeb, Markus, Wöhrle, Simon, Bergner, Andreas, Bruchhaus, Jens, Ciftci, Tuncay, Dahmann, Georg, Dettling, Maike, Döbel, Sandra, Fuchs, Julian E., Geist, Leonhard, Hela, Wolfgang, Kofink, Christiane, Kousek, Roland, Moser, Franziska, Puchner, Teresa, Rumpel, Klaus, Scharnweber, Maximilian, Werni, Patrick, Wolkerstorfer, Bernhard, Breitsprecher, Dennis, Baaske, Philipp, Pearson, Mark, McConnell, Darryl B., Böttcher, Jark
Published in ChemMedChem (06.05.2021)
Published in ChemMedChem (06.05.2021)
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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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An efficient Negishi cross-coupling reaction catalyzed by nickel(II) and diethyl phosphite
Gavryushin, Andrei, Kofink, Christiane, Manolikakes, Georg, Knochel, Paul
Published in Tetrahedron (07.08.2006)
Published in Tetrahedron (07.08.2006)
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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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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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