Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition von 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

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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach von 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

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Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent von 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

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Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket von Scheufler, Clemens, Möbitz, Henrik, Gaul, Christoph, Ragot, Christian, Be, Céline, Fernández, César, Beyer, Kim S, Tiedt, Ralph, Stauffer, Frédéric

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Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach von 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

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DOT1L inhibition is lethal for multiple myeloma due to perturbation of the endoplasmic reticulum stress pathway von 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

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Synthetic Analogues of Migrastatin That Inhibit Mammary Tumor Metastasis in Mice von Shan, Dandan, Chen, Lin, Njardarson, Jon T., Gaul, Christoph, Ma, Xiaojing, Danishefsky, Samuel J., Huang, Xin-Yun

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Discovery of Potent Cell Migration Inhibitors through Total Synthesis:  Lessons from Structure−Activity Studies of (+)-Migrastatin von Njardarson, Jón T, Gaul, Christoph, Shan, Dandan, Huang, Xin-Yun, Danishefsky, Samuel J

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The Migrastatin Family:  Discovery of Potent Cell Migration Inhibitors by Chemical Synthesis von 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

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En route to the total synthesis of tashironin: on the exercise of stereochemical control by a methyl group in mediating remote cyclization reactions von Cook, Silas P., Gaul, Christoph, Danishefsky, Samuel J.

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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-Hydro... von Gaul, Christoph, Schärer, Kaspar, Seebach, Dieter

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A Valine-Derived Lithiated 3-Methylthiomethyl-1,3-oxazolidin-2-one for Enantioselective Nucleophilic Hydroxymethylation, Formylation, and Alkoxycarbonylation of Aldehydes von Gaul, Christoph, Seebach, Dieter

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Evolution of Novartis’ Small Molecule Screening Deck Design von 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

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Novel inhibitors of the histone methyltransferase DOT1L show potent antileukemic activity in patient-derived xenografts von 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.

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Conjugate Addition of Lithiated (S)-4-Isopropyl-3- [(methylthio)methyl]-5,5-diphenyloxazolidin-2-one to Cinnamoyl Derivatives: Preparation of Enantiomerically Pure 1,4-Diols von Gaul, Christoph, Seebach, Dieter

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Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia von 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.

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Abstract 1770: A new DOT1L inhibitor with in vivo activity in mouse models of MLL-translocated leukemia von 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

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New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse von 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

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Approaches to selective fibroblast growth factor receptor 4 inhibition through targeting the ATP-pocket middle-hinge region von Fairhurst, Robin A, Knoepfel, Thomas, Leblanc, Catherine, Buschmann, Nicole, Gaul, Christoph, Blank, Jutta, Galuba, Inga, Trappe, Jörg, Zou, Chao, Voshol, Johannes, Genick, Christine, Brunet-Lefeuvre, Peggy, Bitsch, Francis, Graus-Porta, Diana, Furet, Pascal

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CHZ868, a Type II JAK2 Inhibitor, Reverses Type I JAK Inhibitor Persistence and Demonstrates Efficacy in Myeloproliferative Neoplasms von Meyer, Sara C., Keller, Matthew D., Chiu, Sophia, Koppikar, Priya, Guryanova, Olga A., Rapaport, Franck, Xu, Ke, Manova, Katia, Pankov, Dmitry, O’Reilly, Richard J., Kleppe, Maria, McKenney, Anna Sophia, Shih, Alan H., Shank, Kaitlyn, Ahn, Jihae, Papalexi, Eftymia, Spitzer, Barbara, Socci, Nick, Viale, Agnes, Mandon, Emeline, Ebel, Nicolas, Andraos, Rita, Rubert, Joëlle, Dammassa, Ernesta, Romanet, Vincent, Dölemeyer, Arno, Zender, Michael, Heinlein, Melanie, Rampal, Raajit, Weinberg, Rona Singer, Hoffman, Ronald, Sellers, William R., Hofmann, Francesco, Murakami, Masato, Baffert, Fabienne, Gaul, Christoph, Radimerski, Thomas, Levine, Ross L.

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