Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
Published in Bioorganic & medicinal chemistry letters (01.07.2013)
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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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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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The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells
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
Published in Cancer research (Chicago, Ill.) (15.07.2007)
Published in Cancer research (Chicago, Ill.) (15.07.2007)
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Tyrosine kinase inhibitors: From rational design to clinical trials
Traxler, Peter, Bold, Guido, Buchdunger, Elisabeth, Caravatti, Giorgio, Furet, Pascal, Manley, Paul, O'Reilly, Terence, Wood, Jeanette, Zimmermann, Juerg
Published in Medicinal research reviews (01.11.2001)
Published in Medicinal research reviews (01.11.2001)
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Conference Proceeding
Hypoxia modulation and radiosensitization by the novel dual EGFR and VEGFR inhibitor AEE788 in spontaneous and related allograft tumor models
Christoph Oehler-Jänne, Wolfram Jochum, Oliver Riesterer, Angela Broggini-Tenzer, Giorgio Caravatti, Van Vuong, Martin Pruschy
Published in Molecular cancer therapeutics (01.09.2007)
Published in Molecular cancer therapeutics (01.09.2007)
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Selective GRB2 SH2 inhibitors as anti‐Ras therapy
Gay, Brigitte, Suarez, Stéphanie, Caravatti, Giorgio, Furet, Pascal, Meyer, Thomas, Schoepfer, Joseph
Published in International journal of cancer (08.10.1999)
Published in International journal of cancer (08.10.1999)
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The Total Synthesis and Biological Assessment of trans-Epothilone A
Altmann, Karl-Heinz, Bold, Guido, Caravatti, Giorgio, Denni, Donatienne, Flörsheimer, Andreas, Schmidt, Alfred, Rihs, Grety, Wartmann, Markus
Published in Helvetica chimica acta (01.11.2002)
Published in Helvetica chimica acta (01.11.2002)
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Journal Article
Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain
Furet, Pascal, Gay, Brigitte, Caravatti, Giorgio, García-Echeverría, Carlos, Rahuel, Joseph, Schoepfer, Joseph, Fretz, Heinz
Published in Journal of medicinal chemistry (27.08.1998)
Published in Journal of medicinal chemistry (27.08.1998)
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Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility
Gay, Brigitte, Suarez, Stéphanie, Weber, Christine, Rahuel, Joseph, Fabbro, Doriano, Furet, Pascal, Caravatti, Giorgio, Schoepfer, Joseph
Published in The Journal of biological chemistry (13.08.1999)
Published in The Journal of biological chemistry (13.08.1999)
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Recent developments in the chemistry and biology of epothilones
Altmann, Karl-Heinz, Cachoux, Frederic, Caravatti, Giorgio, Isarno, Thomas, Wartmann, Markus
Published in ARKIVOC (15.09.2006)
Published in ARKIVOC (15.09.2006)
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Web Resource
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
Meyer, T, Regenass, U, Fabbro, D, Alteri, E, Rösel, J, Müller, M, Caravatti, G, Matter, A
Published in International journal of cancer (15.05.1989)
Published in International journal of cancer (15.05.1989)
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Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands
Rahuel, Joseph, Garcı́a-Echeverrı́a, Carlos, Furet, Pascal, Strauss, André, Caravatti, Giorgio, Fretz, Heinz, Schoepfer, Joseph, Gay, Brigitte
Published in Journal of molecular biology (19.06.1998)
Published in Journal of molecular biology (19.06.1998)
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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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Potent Antagonists of the SH2 Domain of Grb2: Optimization of the X+1 Position of 3-Amino-Z-Tyr(PO3H2)-X+1-Asn-NH2
García-Echeverría, Carlos, Furet, Pascal, Gay, Brigitte, Fretz, Heinz, Rahuel, Joseph, Schoepfer, Joseph, Caravatti, Giorgio
Published in Journal of medicinal chemistry (21.05.1998)
Published in Journal of medicinal chemistry (21.05.1998)
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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
Manley, Paul W, Caravatti, Giorgio, Furet, Pascal, Roesel, Johannes, Tran, Phi, Wagner, Trixie, Wartmann, Markus
Published in Biochemistry (Easton) (25.09.2018)
Published in Biochemistry (Easton) (25.09.2018)
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AEE788
Traxler, Peter, Allegrini, Peter R., Brandt, Ralf, Brueggen, Josef, Cozens, Robert, Fabbro, Doriano, Grosios, Konstantina, Lane, Heidi A., McSheehy, Paul, Mestan, Jürgen, Meyer, Thomas, Tang, Careen, Wartmann, Markus, Wood, Jeanette, Caravatti, Giorgio
Published in Cancer research (Chicago, Ill.) (15.07.2004)
Published in Cancer research (Chicago, Ill.) (15.07.2004)
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Epothilones and Their Analogs – Potential New Weapons in the Fight Against Cancer
Karl-Heinz Altmann, Guido Bold, Giorgio Caravatti, Nicole End, Andreas Flörsheimer, Vito Guagnano, Terence O'Reilly, Markus Wartmann
Published in Chimia (01.01.2000)
Published in Chimia (01.01.2000)
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Structural basis for specificity of Grb2-SH2 revealed by a novel ligand binding mode
Rahuel, J, Gay, B, Erdmann, D, Strauss, A, Garcia-Echeverría, C, Furet, P, Caravatti, G, Fretz, H, Schoepfer, J, Grütter, M G
Published in Nature structural biology (01.07.1996)
Published in Nature structural biology (01.07.1996)
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