Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor
Maira, Sauveur-Michel, Pecchi, Sabina, Huang, Alan, Burger, Matthew, Knapp, Mark, Sterker, Dario, Schnell, Christian, Guthy, Daniel, Nagel, Tobi, Wiesmann, Marion, Brachmann, Saskia, Fritsch, Christine, Dorsch, Marion, Chène, Patrick, Shoemaker, Kevin, De Pover, Alain, Menezes, Daniel, Martiny-Baron, Georg, Fabbro, Doriano, Wilson, Christopher J, Schlegel, Robert, Hofmann, Francesco, García-Echeverría, Carlos, Sellers, William R, Voliva, Charles F
Published in Molecular cancer therapeutics (01.02.2012)
Published in Molecular cancer therapeutics (01.02.2012)
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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
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)
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Journal Article
Tetra-substituted imidazoles as a new class of inhibitors of the p53–MDM2 interaction
Vaupel, Andrea, Bold, Guido, De Pover, Alain, Stachyra-Valat, Thérèse, Hergovich Lisztwan, Joanna, Kallen, Joerg, Masuya, Keiichi, Furet, Pascal
Published in Bioorganic & medicinal chemistry letters (01.05.2014)
Published in Bioorganic & medicinal chemistry letters (01.05.2014)
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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)
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Journal Article
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors
Gerspacher, Marc, Furet, Pascal, Pissot-Soldermann, Carole, Gaul, Christoph, Holzer, Philipp, Vangrevelinghe, Eric, Lang, Marc, Erdmann, Dirk, Radimerski, Thomas, Regnier, Catherine H., Chene, Patrick, Pover, Alain De, Hofmann, Francesco, Baffert, Fabienne, Buhl, Thomas, Aichholz, Reiner, Blasco, Francesca, Endres, Ralf, Trappe, Jörg, Drueckes, Peter
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Study of the Selectivity of Insulin-Like Growth Factor-1 Receptor (IGF1R) Inhibitors
Chène, Patrick, Hau, Jean-Christophe, Blechschmidt, Anke, Fontana, Patricia, Bohn, Jacqueline, Zimmermann, Catherine, Pover, Alain De, Erdmann, Dirk
Published in The open enzyme inhibition journal (11.07.2010)
Published in The open enzyme inhibition journal (11.07.2010)
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Journal Article
Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials
Fritsch, Christine, Huang, Alan, Chatenay-Rivauday, Christian, Schnell, Christian, Reddy, Anupama, Liu, Manway, Kauffmann, Audrey, Guthy, Daniel, Erdmann, Dirk, De Pover, Alain, Furet, Pascal, Gao, Hui, Ferretti, Stephane, Wang, Youzhen, Trappe, Joerg, Brachmann, Saskia M, Maira, Sauveur-Michel, Wilson, Christopher, Boehm, Markus, Garcia-Echeverria, Carlos, Chene, Patrick, Wiesmann, Marion, Cozens, Robert, Lehar, Joseph, Schlegel, Robert, Caravatti, Giorgio, Hofmann, Francesco, Sellers, William R
Published in Molecular cancer therapeutics (01.05.2014)
Published in Molecular cancer therapeutics (01.05.2014)
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Journal Article
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53–MDM2 interaction
Furet, Pascal, Chène, Patrick, De Pover, Alain, Valat, Thérèse Stachyra, Lisztwan, Joanna Hergovich, Kallen, Joerg, Masuya, Keiichi
Published in Bioorganic & medicinal chemistry letters (15.05.2012)
Published in Bioorganic & medicinal chemistry letters (15.05.2012)
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Journal Article
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805
Baffert, Fabienne, Régnier, Catherine H, De Pover, Alain, Pissot-Soldermann, Carole, Tavares, Gisele A, Blasco, Francesca, Brueggen, Josef, Chène, Patrick, Drueckes, Peter, Erdmann, Dirk, Furet, Pascal, Gerspacher, Marc, Lang, Marc, Ledieu, David, Nolan, Lynda, Ruetz, Stephan, Trappe, Joerg, Vangrevelinghe, Eric, Wartmann, Markus, Wyder, Lorenza, Hofmann, Francesco, Radimerski, Thomas
Published in Molecular cancer therapeutics (01.07.2010)
Published in Molecular cancer therapeutics (01.07.2010)
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Journal Article
Corrigendum to “Tetra-substituted imidazoles as a new class of inhibitors of the p53–MDM2 interaction” [Bioorg. Med. Chem. Lett. 24 (9) (2014) 2110–2114]
Vaupel, Andrea, Bold, Guido, De Pover, Alain, Stachyra-Valat, Thérèse, Hergovich Lisztwan, Joanna, Kallen, Joerg, Masuya, Keiichi, Furet, Pascal
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
Published in Bioorganic & medicinal chemistry letters (15.03.2015)
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Journal Article
Leveraging the contribution of thermodynamics in drug discovery with the help of fluorescence-based thermal shift assays
Hau, Jean Christophe, Fontana, Patrizia, Zimmermann, Catherine, De Pover, Alain, Erdmann, Dirk, Chène, Patrick
Published in Journal of biomolecular screening (01.06.2011)
Published in Journal of biomolecular screening (01.06.2011)
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Journal Article
Abstract 3748: NVP-BYL719, a novel PI3Kalpha selective inhibitor with all the characteristics required for clinical development as an anti-cancer agent
Fritsch, Christine M., Schnell, Christian, Chatenay-Rivauday, Christian, Guthy, Daniel A., Pover, Alain De, Wartmann, Markus, Brachmann, Saskia, Maira, Sauveur-Michel, Huang, Alan, Quadt, Cornelia, Hofmann, Francesco, Caravatti, Giorgio
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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Abstract 1922: 2-Aminothiazoles as potent and selective PI3Kalpha inhibitors: Discovery of NVP-BYL719 and structural basis for the isoform selectivity
Caravatti, Giorgio, Guagnano, Vito, Fairhurst, Robin, Imbach, Patricia, Bruce, Ian, Knapp, Mark, Furet, Pascal, Fritsch, Christine, Pover, Alain De, Blasco, Francesca, Blanz, Joachim, Seiler, Frank H., Fabbro, Doriano, Lang, Marc
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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Journal Article
Genetic Resistance to JAK2 Enzymatic Inhibitors Is Overcome by HSP90 Inhibition
Weigert, Oliver, Lane, Andrew A., Bird, Liat, Kopp, Nadja, Toms, Angela V, Gaul, Christoph, Vangrevelinghe, Eric, De Pover, Alain, Regnier, Catherine H., Erdmann, Dirk, Hofmann, Francesco, Eck, Michael, Kung, Andrew L., Radimerski, Thomas, Weinstock, David M
Published in Blood (18.11.2011)
Published in Blood (18.11.2011)
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Journal Article
Simultaneous protein expression and modification: an efficient approach for production of unphosphorylated and biotinylated receptor tyrosine kinases by triple infection in the baculovirus expression system
Erdmann, Dirk, Zimmermann, Catherine, Fontana, Patrizia, Hau, Jean-Christophe, De Pover, Alain, Chène, Patrick
Published in Journal of biomolecular techniques (01.04.2010)
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Published in Journal of biomolecular techniques (01.04.2010)
Journal Article
Novel, Potent and Selective JAK2 Inhibitors
Radimerski, Thomas, Baffert, Fabienne, Regnier, Catherine H., De Pover, Alain, Pissot, Carole, Gerspacher, Marc, Brueggen, Josef, Tavares, Gisele, Blasco, Francesca, Ledieu, David, Nolan, Lynda, Ruetz, Stephan, Chene, Patrick, Erdmann, Dirk, Drueckes, Peter, Furet, Pascal, Lang, Marc, Trappe, Joerg, Vangrevelinghe, Eric, Wartmann, Markus, Hofmann, Francesco
Published in Blood (20.11.2009)
Published in Blood (20.11.2009)
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Journal Article
Kinetic Study of Human Full-Length Wild-Type JAK2 and V617F Mutant Proteins
Erdmann, Dirk, Allard, Bertrand, Bohn, Jacqueline, De Pover, Alain, Floersheimer, Andreas, Fontana, Patrizia, Gerspacher, Marc, Hau, Jean Christophe, Hofmann, Francesco, Radimerski, Thomas, Wille, Roman, Zimmermann, Catherine, Chene, Patrick
Published in The open enzyme inhibition journal (02.01.2009)
Published in The open enzyme inhibition journal (02.01.2009)
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Journal Article