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Probing Protein-Ligand Methyl-π Interaction Geometries through Chemical Shift Measurements of Selectively Labeled Methyl Groups Beier, Andreas; Platzer, Gerald; Hofurthner, Theresa; Ptaszek, Aleksandra L.; Lichtenecker, Roman J.; Geist, Leonhard; Fuchs, Julian E.; McConnell, Darryl B.; Mayer, Moriz; Konrat, Robert 分享 收藏
KRASmulti inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRASG12V mutations and KRAS wild-type amplifications Tedeschi, Antonio; Peng, David H.; Schischlik, Fiorella; Herdeis, Lorenz; Schaaf, Otmar; Santoro, Valeria; Gerlach, Daniel; Savarese, Fabio; Lipp, Jesse; Haslinger, Christian; Rocchetti, Francesca; Popow, Johannes; Huber, Heinrich J.; Wilding, Birgit; Treu, Matthias; Fuchs, Julian; Broeker, Joachim; Wunber, Tobias; Gmachl, Michael; Rumpel, Klaus; Rees, Matthew; Ron, Melissa; Roth, Jennifer; Williams, Mariah; Deckard, Charles; Ramamoorthy, Vandhana; Daniele, Joseph R.; Ajani, Jaffer A.; Meric-Bernstam, Funda; Kopetz, Scott; Kim, Michael; Gibbons, Don L.; Vellano, Christopher P.; Marszalek, Joseph R.; Heffernan, Timothy P.; McConnell, Darryl; Pearson, Mark; Kraut, Norbert; Rudolph, Dorothea 分享 收藏
KRASmulti inhibitor BI 3706674, an orally bioavailable, direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRASG12V-driven preclinical models Peng, David Hwa; Tedeschi, Antonio; Herdeis, Lorenz; Schaaf, Otmar; Savarese, Fabio; Rocchetti, Francesca; Popow, Johannes; Huber, Heinrich J.; Wilding, Birgit; Treu, Matthias; Fuchs, Julian; Broeker, Joachim; Wunberg, Tobias; Schischlik, Firoella; Lipp, Jesse; Williams, Mariah; Chandler, Vaness; Deckard, Charles E.; Ramamoorthy, Vandhana; Daniele, Joseph R.; Kopetz, Scott; Kim, Michael; Gibbons, Don L.; Vellano, Christopher P.; Marszalek, Joseph R.; Heffernan, TImothy P.; McConnell, Darryl; Pearson, Mark; Kraut, Norbert; Rudolph, Dorothea 分享 收藏
Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens Schischlik, Fiorella; Tedeschi, Antonio; Rudolph, Dorothea; Gerlach, Daniel; Wilding, Birgit; Treu, Matthias; Fuchs, Julian; Herdeis, Lorenz; Broeker, Joachim; Wunberg, Tobias; Boghossian, Andrew S.; Rees, Matthew G.; Ronan, Melissa M.; Roth, Jennifer A.; McConnell, Darryl; Pearson, Mark; Kraut, Norbert; Haslinger, Christian; Lipp, Jesse 分享 收藏
BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical models Peng, David H.; Tedeschi, Antonio; Herdeis, Lorenz; Savarese, Fabio; Rocchetti, Francesca; Johannes, Popow; Huber, Heinrich J.; Melillo, Nicola; Dickinson, Jake; Mistry, Hitesh B.; Wilding, Birgit; Treu, Matthias; Fuchs, Julian; Broker, Joachim; Wunberg, Tobias; Schischlik, Fiorella; Lipp, Jesse; Ramamoorthy, Vandhana; Daniele, Joseph R.; Kopetz, Scott; Kim, Michael; Gibbons, Don L.; Vellano, Christopher P.; Marszalek, Joseph R.; Heffernan, Timothy P.; McConnell, Darryl; Pearson, Mark; Kraut, Norbert; Rudolph, Dorothea 分享 收藏
BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validates wild-type amplified KRAS as a therapeutic target Tedeschi, Antonio; Herdeis, Lorenz; Santoro, Valeria; Savarese, Fabio; Wilding, Birgit; Treu, Matthias; Fuchs, Julian; Broker, Joachim; Wunberg, Tobias; Gmachl, Michael; Klaus, Rumpel; Schischlik, Fiorella; Lipp, Jesse; Peng, David H.; Williams, Mariah; Deckard, Charles; Ramamoorthy, Vandhana; Daniele, Joseph R.; Ajani, Jaffer A.; Meric-Bernstam, Funda; Vellano, Christopher R.; Marszalek, Joseph R.; Heffernan, Timothy P.; McConnell, Darryl; Pearson, Mark; Kraut, Norbert; Rudolph, Dorothea 分享 收藏
Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments Martinelli, Paola; Schaaf, Otmar; Mantoulidis, Andreas; Martin, Laetitia J.; Fuchs, Julian E.; Bader, Gerd; Gollner, Andreas; Wolkerstorfer, Bernhard; Rogers, Catherine; Balikci, Esra; Lipp, Jesse J.; Mischerikow, Nikolai; Doebel, Sandra; Gerstberger, Thomas; Sommergruber, Wolfgang; Huber, Kilian V. M.; Boettcher, Jark 分享 收藏
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo Kofink, Christiane; Trainor, Nicole; Mair, Barbara; Woehrle, Simon; Wurm, Melanie; Mischerikow, Nikolai; Roy, Michael J.; Bader, Gerd; Greb, Peter; Garavel, Geraldine; 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 分享 收藏
Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling 发现对HER2外显子20插入驱动的肿瘤有效的和选择性的HER2抑制剂，其保留野生型EGFR信号传导 Wilding, Birgit; Scharn, Dirk; Boese, Dietrich; Baum, Anke; Santoro, Valeria; Chetta, Paolo; Schnitzer, Renate; Botesteanu, Dana A.; Reiser, Christoph; Kornigg, Stefan; Knesl, Petr; Hoermann, Alexandra; Koeferle, Anna; Corcokovic, Maja; Lieb, Simone; Scholz, Guido; Bruchhaus, Jens; Spina, Markus; Balla, Josef; Peric-Simov, Biljana; Zimmer, Jasmin; Mitzner, Sophie; Fett, Thomas N.; Beran, Alexandra; Lamarre, Lyne; Gerstberger, Thomas; Gerlach, Daniel; Bauer, Markus; Bergner, Andreas; Schlattl, Andreas; Bader, Gerd; Treu, Matthias; Engelhardt, Harald; Zahn, Stephan; Fuchs, Julian E.; Zuber, Johannes; Ettmayer, Peter; Pearson, Mark; Petronczki, Mark; Kraut, Norbert; McConnell, Darryl B.; Solca, Flavio; Neumuller, Ralph A. 分享 收藏
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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; Woehrle, Simon; Bergner, Andreas; Bruchhaus, Jens; Ciftci, Tuncay; Dahmann, Georg; Dettling, Maike; Doebel, 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.; Boettcher, Jark 分享 收藏
PI by NMR: Probing CH-π Interactions in Protein-Ligand Complexes by NMR Spectroscopy Platzer, Gerald; Mayer, Moriz; Beier, Andreas; Brueschweiler, Sven; Fuchs, Julian E.; Engelhardt, Harald; Geist, Leonhard; Bader, Gerd; Schoerghuber, Julia; Lichtenecker, Roman; Wolkerstorfer, Bernhard; Kessler, Dirk; McConnell, Darryl B.; Konrat, Robert 分享 收藏
Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors Engelhardt, Harald; Boese, Dietrich; Petronczki, Mark; Scharn, Dirk; Bader, Gerd; Baum, Anke; Bergner, Andreas; Chong, Eugene; Doebel, 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; Stadtmueller, Heinz; Tan, Zhulin; Wunberg, Tobias; Zoephel, Andreas; McConnell, Darryl B. 分享 收藏
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3 Boettcher, Jark; Dilworth, David; Reiser, Ulrich; Neumueller, Ralph A.; Schleicher, Michael; Petronczki, Mark; Zeeb, Markus; Mischerikow, Nikolai; Allali-Hassani, Abdellah; Szewczyk, Magdalena M.; Li, Fengling; Kennedy, Steven; Vedadi, Masoud; Barsyte-Lovejoy, Dalia; Brown, Peter J.; Huber, Kilian V. M.; Rogers, Catherine M.; Wells, Carrow, I; Fedorov, Oleg; Rumpel, Klaus; Zoephel, Andreas; Mayer, Moriz; Wunberg, Tobias; Boese, Dietrich; Zahn, Stephan; Arnhof, Heribert; Berger, Helmut; Reiser, Christoph; Hoermann, Alexandra; Krammer, Teresa; Corcokovic, Maja; Sharps, Bernadette; Winkler, Sandra; Haering, Daniela; Cockcroft, Xiao-Ling; Fuchs, Julian E.; Muellauer, Barbara; Weiss-Puxbaum, Alexander; Gerstberger, Thomas; Boehmelt, Guido; Vakoc, Christopher R.; Arrowsmith, Cheryl H.; Pearson, Mark; McConnell, Darryl B. 分享 收藏
Targeted Synthesis of Complex Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors Gollner, Andreas; Weinstabl, Harald; Fuchs, Julian E.; Rudolph, Dorothea; Garavel, Geraldine; Hofbauer, Karin S.; Karolyi-Oezguer, Jale; Gmaschitz, Gerhard; Hela, Wolfgang; Kerres, Nina; Grondal, Elisabeth; Werni, Patrick; Ramharter, Juergen; Broeker, Joachim; McConnell, Darryl B. 分享 收藏
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Discovery of a small-molecule inhibitor of specific serine residue BAD phosphorylation Pandey, Vijay; Wang, Baocheng; Mohan, Chakrabhavi Dhananjaya; Raquib, Ainiah Rushdiana; Rangappa, Shobith; Srinivasa, Venkatachalaiah; Fuchs, Julian E.; Girish, Kesturu S.; Zhu, Tao; Bender, Andreas; Ma, Lan; Yin, Zhinan; Basappa; Rangappa, Kanchugarakoppal S.; Lobie, Peter E. 分享 收藏
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