Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation von Furet, Pascal, Guagnano, Vito, Fairhurst, Robin A., Imbach-Weese, Patricia, Bruce, Ian, Knapp, Mark, Fritsch, Christine, Blasco, Francesca, Blanz, Joachim, Aichholz, Reiner, Hamon, Jacques, Fabbro, Doriano, Caravatti, Giorgio

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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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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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The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells von AKENO-STUART, Nagako, CROYLE, Michelle, CARAVATTI, Giorgio, FABBRO, Doriano, LANE, Heidi A, FAGIN, James A, KNAUF, Jeffrey A, MALAGUARNERA, Roberta, VITAGLIANO, Donata, SANTORO, Massimo, STEPHAN, Christine, GROSIOS, Konstantina, WARTMANN, Markus, COZENS, Robert

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Tyrosine kinase inhibitors: From rational design to clinical trials von Traxler, Peter, Bold, Guido, Buchdunger, Elisabeth, Caravatti, Giorgio, Furet, Pascal, Manley, Paul, O'Reilly, Terence, Wood, Jeanette, Zimmermann, Juerg

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Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials von 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

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Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models von Christoph Oehler-Jänne, Wolfram Jochum, Oliver Riesterer, Angela Broggini-Tenzer, Giorgio Caravatti, Van Vuong, Martin Pruschy

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Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its Predominant Metabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy von Manley, Paul W, Caravatti, Giorgio, Furet, Pascal, Roesel, Johannes, Tran, Phi, Wagner, Trixie, Wartmann, Markus

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Selective GRB2 SH2 inhibitors as anti‐Ras therapy von Gay, Brigitte, Suarez, Stéphanie, Caravatti, Giorgio, Furet, Pascal, Meyer, Thomas, Schoepfer, Joseph

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The Total Synthesis and Biological Assessment of trans-Epothilone A von Altmann, Karl-Heinz, Bold, Guido, Caravatti, Giorgio, Denni, Donatienne, Flörsheimer, Andreas, Schmidt, Alfred, Rihs, Grety, Wartmann, Markus

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Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain von Furet, Pascal, Gay, Brigitte, Caravatti, Giorgio, García-Echeverría, Carlos, Rahuel, Joseph, Schoepfer, Joseph, Fretz, Heinz

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Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor von 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

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Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites von Manley, Paul W, Caravatti, Giorgio, Furet, Pascal, Roesel, Johannes, Tran, Phi, Wagner, Trixie

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A derivative of staurosporine (CGP 41 251) shows selectivity for protein kinase C inhibition and In vitro anti‐proliferative as well as In vivo anti‐tumor activity von Meyer, Thomas, Regenass, Urs, Fabbro, Doriano, Alteri, Enrica, Röusel, Johannes, Möller, Marcel, Caravatti, Giorgio, Matter, Alex

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Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility von Gay, Brigitte, Suarez, Stéphanie, Weber, Christine, Rahuel, Joseph, Fabbro, Doriano, Furet, Pascal, Caravatti, Giorgio, Schoepfer, Joseph

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AEE788: A dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity von TRAXLER, Peter, ALLEGRINI, Peter R, MEYER, Thomas, TANG, Careen, WARTMANN, Markus, WOOD, Jeanette, CARAVATTI, Giorgio, BRANDT, Ralf, BRUEGGEN, Josef, COZENS, Robert, FABBRO, Doriano, GROSIOS, Konstantina, LANE, Heidi A, MCSHEEHY, Paul, MESTAN, Jürgen

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Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands von Rahuel, Joseph, Garcı́a-Echeverrı́a, Carlos, Furet, Pascal, Strauss, André, Caravatti, Giorgio, Fretz, Heinz, Schoepfer, Joseph, Gay, Brigitte

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Recent developments in the chemistry and biology of epothilones von Altmann, Karl-Heinz, Cachoux, Frederic, Caravatti, Giorgio, Isarno, Thomas, Wartmann, Markus

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Potent Antagonists of the SH2 Domain of Grb2:  Optimization of the X+1 Position of 3-Amino-Z-Tyr(PO3H2)-X+1-Asn-NH2 von García-Echeverría, Carlos, Furet, Pascal, Gay, Brigitte, Fretz, Heinz, Rahuel, Joseph, Schoepfer, Joseph, Caravatti, Giorgio

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Entry into a new class of protein kinase inhibitors by pseudo ring design von Furet, Pascal, Caravatti, Giorgio, Guagnano, Vito, Lang, Marc, Meyer, Thomas, Schoepfer, Joseph

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