Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition
Weigert, Oliver, Lane, Andrew A, Bird, Liat, Kopp, Nadja, Chapuy, Bjoern, van Bodegom, Diederik, Toms, Angela V, Marubayashi, Sachie, Christie, Amanda L, McKeown, Michael, Paranal, Ronald M, Bradner, James E, Yoda, Akinori, Gaul, Christoph, Vangrevelinghe, Eric, Romanet, Vincent, Murakami, Masato, Tiedt, Ralph, Ebel, Nicolas, Evrot, Emeline, De Pover, Alain, Régnier, Catherine H, Erdmann, Dirk, Hofmann, Francesco, Eck, Michael J, Sallan, Stephen E, Levine, Ross L, Kung, Andrew L, Baffert, Fabienne, Radimerski, Thomas, Weinstock, David M
Published in The Journal of experimental medicine (13.02.2012)
Published in The Journal of experimental medicine (13.02.2012)
Get full text
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)
Get full text
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)
Get full text
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)
Get full text
Journal Article
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent
Andraos, Rita, Qian, Zhiyan, Bonenfant, Débora, Rubert, Joëlle, Vangrevelinghe, Eric, Scheufler, Clemens, Marque, Fanny, Régnier, Catherine H, De Pover, Alain, Ryckelynck, Hugues, Bhagwat, Neha, Koppikar, Priya, Goel, Aviva, Wyder, Lorenza, Tavares, Gisele, Baffert, Fabienne, Pissot-Soldermann, Carole, Manley, Paul W, Gaul, Christoph, Voshol, Hans, Levine, Ross L, Sellers, William R, Hofmann, Francesco, Radimerski, Thomas
Published in Cancer discovery (01.06.2012)
Published in Cancer discovery (01.06.2012)
Get full text
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)
Get full text
Journal Article
Synthetic Analogues of Migrastatin That Inhibit Mammary Tumor Metastasis in Mice
Shan, Dandan, Chen, Lin, Njardarson, Jon T., Gaul, Christoph, Ma, Xiaojing, Danishefsky, Samuel J., Huang, Xin-Yun
Published in Proceedings of the National Academy of Sciences - PNAS (08.03.2005)
Published in Proceedings of the National Academy of Sciences - PNAS (08.03.2005)
Get full text
Journal Article
Discovery of Potent Cell Migration Inhibitors through Total Synthesis: Lessons from Structure−Activity Studies of (+)-Migrastatin
Njardarson, Jón T, Gaul, Christoph, Shan, Dandan, Huang, Xin-Yun, Danishefsky, Samuel J
Published in Journal of the American Chemical Society (04.02.2004)
Published in Journal of the American Chemical Society (04.02.2004)
Get full text
Journal Article
The Migrastatin Family: Discovery of Potent Cell Migration Inhibitors by Chemical Synthesis
Gaul, Christoph, Njardarson, Jón T, Shan, Dandan, Dorn, David C, Wu, Kai-Da, Tong, William P, Huang, Xin-Yun, Moore, Malcolm A. S, Danishefsky, Samuel J
Published in Journal of the American Chemical Society (15.09.2004)
Published in Journal of the American Chemical Society (15.09.2004)
Get full text
Journal Article
Lithiated 4-Isopropyl-3-(methylthiomethyl)-5,5-diphenyloxazolidin-2-one: A Chiral Formyl Anion Equivalent for Enantioselective Preparations of 1,2-Diols, 2-Amino Alcohols, 2-Hydroxy Esters, and 4-Hydroxy-2-alkenoates
Gaul, Christoph, Schärer, Kaspar, Seebach, Dieter
Published in Journal of organic chemistry (04.05.2001)
Published in Journal of organic chemistry (04.05.2001)
Get full text
Journal Article
Evolution of Novartis’ Small Molecule Screening Deck Design
Schuffenhauer, Ansgar, Schneider, Nadine, Hintermann, Samuel, Auld, Douglas, Blank, Jutta, Cotesta, Simona, Engeloch, Caroline, Fechner, Nikolas, Gaul, Christoph, Giovannoni, Jerome, Jansen, Johanna, Joslin, John, Krastel, Philipp, Lounkine, Eugen, Manchester, John, Monovich, Lauren G, Pelliccioli, Anna Paola, Schwarze, Manuel, Shultz, Michael D, Stiefl, Nikolaus, Baeschlin, Daniel K
Published in Journal of medicinal chemistry (10.12.2020)
Published in Journal of medicinal chemistry (10.12.2020)
Get full text
Journal Article
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)
Get full text
Journal Article
Computational, ReactIR-, and NMR-Spectroscopic Investigations on the Chiral Formyl Anion EquivalentN-(α-Lithiomethylthiomethyl)-4-isopropyl-5,5-diphenyloxazolidin-2-one and Related Compounds
Gaul, Christoph, Arvidsson, Per I., Bauer, Walter, Gawley, Robert E., Seebach, Dieter
Published in Chemistry : a European journal (01.10.2001)
Published in Chemistry : a European journal (01.10.2001)
Get full text
Journal Article
From Synthetic Methods to gamma-Peptides – From Chemistry to Biology
Dieter Seebach, Albert K. Beck, Meinrad Brenner, Christoph Gaul, Alexander Heckel
Published in Chimia (01.01.2001)
Published in Chimia (01.01.2001)
Get full text
Journal Article
Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia
Wu, Shuo-Chieh, Li, Loretta S., Kopp, Nadja, Montero, Joan, Chapuy, Bjoern, Yoda, Akinori, Christie, Amanda L., Liu, Huiyun, Christodoulou, Alexandra, van Bodegom, Diederik, van der Zwet, Jordy, Layer, Jacob V., Tivey, Trevor, Lane, Andrew A., Ryan, Jeremy A., Ng, Samuel Y., DeAngelo, Daniel J., Stone, Richard M., Steensma, David, Wadleigh, Martha, Harris, Marian, Mandon, Emeline, Ebel, Nicolas, Andraos, Rita, Romanet, Vincent, Dölemeyer, Arno, Sterker, Dario, Zender, Michael, Rodig, Scott J., Murakami, Masato, Hofmann, Francesco, Kuo, Frank, Eck, Michael J., Silverman, Lewis B., Sallan, Stephen E., Letai, Anthony, Baffert, Fabienne, Vangrevelinghe, Eric, Radimerski, Thomas, Gaul, Christoph, Weinstock, David M.
Published in Cancer cell (13.07.2015)
Published in Cancer cell (13.07.2015)
Get full text
Journal Article
Abstract 1770: A new DOT1L inhibitor with in vivo activity in mouse models of MLL-translocated leukemia
Weiss, Andreas, Stauffer, Frederic, Clemens, Clemens, Möbitz, Henrik, Ragot, Christian, Beyer, Kim S., Calkins, Keith, Thoma, Claudio, Guthy, Daniel, Kiffe, Michael, Van Eerdenbrugh, Bernard, Sellers, William R., Hofmann, Francesco, Tiedt, Ralph, Gaul, Christoph
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Get full text
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)
Get full text
Journal Article