Novel inhibitors of the histone methyltransferase DOT1L show potent antileukemic activity in patient-derived xenografts
Perner, Florian, Gadrey, Jayant Y., Xiong, Yijun, Hatton, Charles, Eschle, Benjamin K., Weiss, Andreas, Stauffer, Frédéric, Gaul, Christoph, Tiedt, Ralph, Perry, Jennifer A., Armstrong, Scott A., Krivtsov, Andrei V.
Published in Blood (22.10.2020)
Published in Blood (22.10.2020)
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Journal Article
PI3K inhibitors for cancer treatment: where do we stand?
Maira, Sauveur-Michel, Stauffer, Frédéric, Schnell, Christian, García-Echeverría, Carlos
Published in Biochemical Society transactions (01.02.2009)
Published in Biochemical Society transactions (01.02.2009)
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Journal Article
Targeting Melanoma with Dual Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitors
Marone, Romina, Erhart, Dominik, Mertz, Ann C, Bohnacker, Thomas, Schnell, Christian, Cmiljanovic, Vladimir, Stauffer, Frédéric, Garcia-Echeverria, Carlos, Giese, Bernd, Maira, Sauveur-Michel, Wymann, Matthias P
Published in Molecular cancer research (01.04.2009)
Published in Molecular cancer research (01.04.2009)
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Journal Article
Imidazo[4,5- c]quinolines as inhibitors of the PI3K/PKB-pathway
Stauffer, Frédéric, Maira, Sauveur-Michel, Furet, Pascal, García-Echeverría, Carlos
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
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Journal Article
A General Strategy for Targeting Drugs to Bone
Jahnke, Wolfgang, Bold, Guido, Marzinzik, Andreas L., Ofner, Silvio, Pellé, Xavier, Cotesta, Simona, Bourgier, Emmanuelle, Lehmann, Sylvie, Henry, Chrystelle, Hemmig, René, Stauffer, Frédéric, Hartwieg, J. Constanze D., Green, Jonathan R., Rondeau, Jean-Michel
Published in Angewandte Chemie International Edition (23.11.2015)
Published in Angewandte Chemie International Edition (23.11.2015)
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Journal Article
Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors
Fairhurst, Robin A., Marsilje, Thomas H., Stutz, Stefan, Boos, Andreas, Niklaus, Michel, Chen, Bei, Jiang, Songchun, Lu, Wenshuo, Furet, Pascal, McCarthy, Clive, Stauffer, Frédéric, Guagnano, Vito, Vaupel, Andrea, Michellys, Pierre-Yves, Schnell, Christian, Jeay, Sébastien
Published in Bioorganic & medicinal chemistry letters (15.04.2016)
Published in Bioorganic & medicinal chemistry letters (15.04.2016)
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Journal Article
Discovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead Finding
Marzinzik, Andreas L., Amstutz, René, Bold, Guido, Bourgier, Emmanuelle, Cotesta, Simona, Glickman, J. Fraser, Götte, Marjo, Henry, Christelle, Lehmann, Sylvie, Hartwieg, J. Constanze D., Ofner, Silvio, Pellé, Xavier, Roddy, Thomas P., Rondeau, Jean-Michel, Stauffer, Frédéric, Stout, Steven J., Widmer, Armin, Zimmermann, Johann, Zoller, Thomas, Jahnke, Wolfgang
Published in ChemMedChem (01.11.2015)
Published in ChemMedChem (01.11.2015)
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Journal Article
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity
Maira, Sauveur-Michel, Stauffer, Frédéric, Brueggen, Josef, Furet, Pascal, Schnell, Christian, Fritsch, Christine, Brachmann, Saskia, Chène, Patrick, De Pover, Alain, Schoemaker, Kevin, Fabbro, Doriano, Gabriel, Daniela, Simonen, Marjo, Murphy, Leon, Finan, Peter, Sellers, William, García-Echeverría, Carlos
Published in Molecular cancer therapeutics (01.07.2008)
Published in Molecular cancer therapeutics (01.07.2008)
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Journal Article
Discovery of novel anticancer therapeutics targeting the PI3K/Akt/mTOR pathway
Maira, Sauveur-Michel, Furet, Pascal, Stauffer, Frédéric
Published in Future medicinal chemistry (01.04.2009)
Published in Future medicinal chemistry (01.04.2009)
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Journal Article
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor
Fairhurst, Robin A., Furet, Pascal, Imbach-Weese, Patricia, Stauffer, Frédéric, Rueeger, Heinrich, McCarthy, Clive, Ripoche, Sebastien, Oswald, Susanne, Arnaud, Bertrand, Jary, Aline, Maira, Michel, Schnell, Christian, Guthy, Daniel A., Wartmann, Markus, Kiffe, Michael, Desrayaud, Sandrine, Blasco, Francesca, Widmer, Toni, Seiler, Frank, Gutmann, Sascha, Knapp, Mark, Caravatti, Giorgio
Published in Journal of medicinal chemistry (23.06.2022)
Published in Journal of medicinal chemistry (23.06.2022)
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Journal Article
Effects of the dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor NVP-BEZ235 on the tumor vasculature: implications for clinical imaging
Schnell, Christian R, Stauffer, Frédéric, Allegrini, Peter R, O'Reilly, Terence, McSheehy, Paul M J, Dartois, Celine, Stumm, Michael, Cozens, Robert, Littlewood-Evans, Amanda, García-Echeverría, Carlos, Maira, Sauveur-Michel
Published in Cancer research (Chicago, Ill.) (15.08.2008)
Published in Cancer research (Chicago, Ill.) (15.08.2008)
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Journal Article
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach
Chen, Chao, Zhu, Hugh, Stauffer, Frédéric, Caravatti, Giorgio, Vollmer, Susanne, Machauer, Rainer, Holzer, Philipp, Möbitz, Henrik, Scheufler, Clemens, Klumpp, Martin, Tiedt, Ralph, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Zhang, Jeff, Gaul, Christoph
Published in ACS medicinal chemistry letters (11.08.2016)
Published in ACS medicinal chemistry letters (11.08.2016)
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Journal Article
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket
Scheufler, Clemens, Möbitz, Henrik, Gaul, Christoph, Ragot, Christian, Be, Céline, Fernández, César, Beyer, Kim S, Tiedt, Ralph, Stauffer, Frédéric
Published in ACS medicinal chemistry letters (11.08.2016)
Published in ACS medicinal chemistry letters (11.08.2016)
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Journal Article
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach
Möbitz, Henrik, Machauer, Rainer, Holzer, Philipp, Vaupel, Andrea, Stauffer, Frédéric, Ragot, Christian, Caravatti, Giorgio, Scheufler, Clemens, Fernandez, Cesar, Hommel, Ulrich, Tiedt, Ralph, Beyer, Kim S, Chen, Chao, Zhu, Hugh, Gaul, Christoph
Published in ACS medicinal chemistry letters (09.03.2017)
Published in ACS medicinal chemistry letters (09.03.2017)
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Journal Article
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse
Stauffer, Frédéric, Weiss, Andreas, Scheufler, Clemens, Möbitz, Henrik, Ragot, Christian, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Van Eerdenbrugh, Bernard, Tiedt, Ralph, Gaul, Christoph
Published in ACS medicinal chemistry letters (12.12.2019)
Published in ACS medicinal chemistry letters (12.12.2019)
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Journal Article
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors
Hoegenauer, Klemens, Soldermann, Nicolas, Stauffer, Frédéric, Furet, Pascal, Graveleau, Nadege, Smith, Alexander B, Hebach, Christina, Hollingworth, Gregory J, Lewis, Ian, Gutmann, Sascha, Rummel, Gabriele, Knapp, Mark, Wolf, Romain M, Blanz, Joachim, Feifel, Roland, Burkhart, Christoph, Zécri, Frédéric
Published in ACS medicinal chemistry letters (11.08.2016)
Published in ACS medicinal chemistry letters (11.08.2016)
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Journal Article
DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway
Dafflon, Caroline, Gaulis, Swann, Barys, Louise, Kapur, Karen, Cornacchione, Vanessa, Schukur, Lina, Bergling, Sebastian, Traggiai, Elisabetta, Jansky, Selina, Hellmann, Leon, Engstler, Barbara Schacher, Kerr, Grainne, de Weck, Antoine, Ruddy, David A, Naumann, Ulrike, Stauffer, Frédéric, Gaul, Christoph, Lin, Ying, Billy, Eric, Weiss, Andreas, Hofmann, Francesco, Ito, Moriko, Tiedt, Ralph
Published in Oncotarget (17.03.2020)
Published in Oncotarget (17.03.2020)
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Journal Article