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)
Get full text
Journal Article
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
Guagnano, Vito, Furet, Pascal, Spanka, Carsten, Bordas, Vincent, Le Douget, Mickaël, Stamm, Christelle, Brueggen, Josef, Jensen, Michael R, Schnell, Christian, Schmid, Herbert, Wartmann, Markus, Berghausen, Joerg, Drueckes, Peter, Zimmerlin, Alfred, Bussiere, Dirksen, Murray, Jeremy, Graus Porta, Diana
Published in Journal of medicinal chemistry (27.10.2011)
Published in Journal of medicinal chemistry (27.10.2011)
Get full text
Journal Article
FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor
Guagnano, Vito, Kauffmann, Audrey, Wöhrle, Simon, Stamm, Christelle, Ito, Moriko, Barys, Louise, Pornon, Astrid, Yao, Yao, Li, Fang, Zhang, Yun, Chen, Zhi, Wilson, Christopher J, Bordas, Vincent, Le Douget, Mickaël, Gaither, L Alex, Borawski, Jason, Monahan, John E, Venkatesan, Kavitha, Brümmendorf, Thomas, Thomas, David M, Garcia-Echeverria, Carlos, Hofmann, Francesco, Sellers, William R, Graus-Porta, Diana
Published in Cancer discovery (01.12.2012)
Published in Cancer discovery (01.12.2012)
Get full text
Journal Article
Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23‐mediated hypophosphatemic rickets
Wöhrle, Simon, Henninger, Christine, Bonny, Olivier, Thuery, Anne, Beluch, Noemie, Hynes, Nancy E, Guagnano, Vito, Sellers, William R, Hofmann, Francesco, Kneissel, Michaela, Graus Porta, Diana
Published in Journal of bone and mineral research (01.04.2013)
Published in Journal of bone and mineral research (01.04.2013)
Get full text
Journal Article
Structural States of Hdm2 and HdmX: X‐ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes
Kallen, Joerg, Izaac, Aude, Chau, Suzanne, Wirth, Emmanuelle, Schoepfer, Joseph, Mah, Robert, Schlapbach, Achim, Stutz, Stefan, Vaupel, Andrea, Guagnano, Vito, Masuya, Keiichi, Stachyra, Therese‐Marie, Salem, Bahaa, Chene, Patrick, Gessier, Francois, Holzer, Philipp, Furet, Pascal
Published in ChemMedChem (17.07.2019)
Published in ChemMedChem (17.07.2019)
Get full text
Journal Article
Fibroblast growth factor receptors as novel therapeutic targets in SNF5-deleted malignant rhabdoid tumors
Wöhrle, Simon, Weiss, Andreas, Ito, Moriko, Kauffmann, Audrey, Murakami, Masato, Jagani, Zainab, Thuery, Anne, Bauer-Probst, Beatrice, Reimann, Flavia, Stamm, Christelle, Pornon, Astrid, Romanet, Vincent, Guagnano, Vito, Brümmendorf, Thomas, Sellers, William R, Hofmann, Francesco, Roberts, Charles W M, Graus Porta, Diana
Published in PloS one (2013)
Published in PloS one (2013)
Get full text
Journal Article
Abstract 1239: NVP-HDM201: Biochemical and biophysical profile of a novel highly potent and selective PPI inhibitor of p53-Mdm2
Stachyra-Valat, Thérèse, Baysang, Frédéric, D’Alessandro, Anne-Cécile, Dirk, Erdmann, Furet, Pascal, Guagnano, Vito, Kallen, Joerg, Leder, Lukas, Mah, Robert, Masuya, Keiichi, Stutz, Stefan, Vaupel, Andrea, Hofmann, Francesco, Chène, Patrick, Jeay, Sébastien, Holzer, Philipp
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Get full text
Journal Article
Discovery of a novel class of highly potent inhibitors of the p53–MDM2 interaction by structure-based design starting from a conformational argument
Furet, Pascal, Masuya, Keiichi, Kallen, Joerg, Stachyra-Valat, Thérèse, Ruetz, Stephan, Guagnano, Vito, Holzer, Philipp, Mah, Robert, Stutz, Stefan, Vaupel, Andrea, Chène, Patrick, Jeay, Sébastien, Schlapbach, Achim
Published in Bioorganic & medicinal chemistry letters (01.10.2016)
Published in Bioorganic & medicinal chemistry letters (01.10.2016)
Get full text
Journal Article
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)
Get full text
Journal Article
The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition
Furet, Pascal, Bordas, Vincent, Le Douget, Mickaël, Salem, Bahaa, Mesrouze, Yannick, Imbach‐Weese, Patricia, Sellner, Holger, Voegtle, Markus, Soldermann, Nicolas, Chapeau, Emilie, Wartmann, Markus, Scheufler, Clemens, Fernandez, Cesar, Kallen, Joerg, Guagnano, Vito, Chène, Patrick, Schmelzle, Tobias
Published in ChemMedChem (06.10.2022)
Published in ChemMedChem (06.10.2022)
Get full text
Journal Article
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor
Vaupel, Andrea, Holzer, Philipp, Ferretti, Stephane, Guagnano, Vito, Kallen, Joerg, Mah, Robert, Masuya, Keiichi, Ruetz, Stephan, Rynn, Caroline, Schlapbach, Achim, Stachyra, Thérèse, Stutz, Stefan, Todorov, Milen, Jeay, Sébastien, Furet, Pascal
Published in Bioorganic & medicinal chemistry letters (01.11.2018)
Published in Bioorganic & medicinal chemistry letters (01.11.2018)
Get full text
Journal Article
Front Cover: The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition (ChemMedChem 19/2022)
Furet, Pascal, Bordas, Vincent, Le Douget, Mickaël, Salem, Bahaa, Mesrouze, Yannick, Imbach‐Weese, Patricia, Sellner, Holger, Voegtle, Markus, Soldermann, Nicolas, Chapeau, Emilie, Wartmann, Markus, Scheufler, Clemens, Fernandez, Cesar, Kallen, Joerg, Guagnano, Vito, Chène, Patrick, Schmelzle, Tobias
Published in ChemMedChem (06.10.2022)
Published in ChemMedChem (06.10.2022)
Get full text
Journal Article
BET bromodomain inhibitors regulate keratinocyte plasticity
Schutzius, Gabi, Kolter, Christian, Bergling, Sebastian, Tortelli, Federico, Fuchs, Florian, Renner, Steffen, Guagnano, Vito, Cotesta, Simona, Rueeger, Heinrich, Faller, Michael, Bouchez, Laure, Salathe, Adrian, Nigsch, Florian, Richards, Shola M., Louis, Malvina, Gruber, Viktoria, Aebi, Alexandra, Turner, Jonathan, Grandjean, Frederic, Li, Jun, Dimitri, Chris, Thomas, Jason R., Schirle, Markus, Blank, Jutta, Drueckes, Peter, Vaupel, Andrea, Tiedt, Ralph, Manley, Paul W., Klopp, Julia, Hemmig, Rene, Zink, Florence, Leroy, Nelly, Carbone, Walter, Roma, Guglielmo, Keller, Caroline Gubser, Dales, Natalie, Beyerbach, Armin, Zimmerlin, Alfred, Bonenfant, Debora, Terranova, Remi, Berwick, Amy, Sahambi, Sukhdeep, Reynolds, Aimee, Jennings, Lori L., Ruffner, Heinz, Tarsa, Peter, Bouwmeester, Tewis, Driver, Vickie, Frederiksen, Mathias, Lohmann, Felix, Kirkland, Susan
Published in Nature chemical biology (01.03.2021)
Published in Nature chemical biology (01.03.2021)
Get full text
Journal Article
Rescue screens with secreted proteins reveal compensatory potential of receptor tyrosine kinases in driving cancer growth
Harbinski, Fred, Craig, Vanessa J, Sanghavi, Sneha, Jeffery, Douglas, Liu, Lijuan, Sheppard, Kelly Ann, Wagner, Sabrina, Stamm, Christelle, Buness, Andreas, Chatenay-Rivauday, Christian, Yao, Yao, He, Feng, Lu, Chris X, Guagnano, Vito, Metz, Thomas, Finan, Peter M, Hofmann, Francesco, Sellers, William R, Porter, Jeffrey A, Myer, Vic E, Graus-Porta, Diana, Wilson, Christopher J, Buckler, Alan, Tiedt, Ralph
Published in Cancer discovery (01.10.2012)
Published in Cancer discovery (01.10.2012)
Get full text
Journal Article
Entry into a new class of protein kinase inhibitors by pseudo ring design
Furet, Pascal, Caravatti, Giorgio, Guagnano, Vito, Lang, Marc, Meyer, Thomas, Schoepfer, Joseph
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
Get full text
Journal Article
Non-Covalent Inhibitors of the 20S Proteasome
Carlos García-Echeverría, Patricia Imbach, Johannes Roesel, Peter Fuerst, Marc Lang, Vito Guagnano, Maria Noorani, Johann Zimmermann, Pascal Furet
Published in Chimia (01.04.2003)
Published in Chimia (01.04.2003)
Get full text
Journal Article
Front Cover: Structural States of Hdm2 and HdmX: X‐ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes (ChemMedChem 14/2019)
Kallen, Joerg, Izaac, Aude, Chau, Suzanne, Wirth, Emmanuelle, Schoepfer, Joseph, Mah, Robert, Schlapbach, Achim, Stutz, Stefan, Vaupel, Andrea, Guagnano, Vito, Masuya, Keiichi, Stachyra, Therese‐Marie, Salem, Bahaa, Chene, Patrick, Gessier, Francois, Holzer, Philipp, Furet, Pascal
Published in ChemMedChem (17.07.2019)
Published in ChemMedChem (17.07.2019)
Get full text
Journal Article
Abstract 4855: Discovery of NVP-HDM201 - First disclosure of a Next-Generation Mdm2 inhibitor with superior characteristics
Holzer, Philipp, Chène, Patrick, Ferretti, Stéphane, Furet, Pascal, Gabriel, Tobias, Gruenenfelder, Bjoern, Guagnano, Vito, Hofmann, Francesco, Kallen, Joerg, Mah, Robert, Masuya, Keiichi, Ramos, Rita, Ruetz, Stephan, Rynn, Caroline, Stachyra-Valat, Thérèse, Stutz, Stefan, Vaupel, Andrea, Jeay, Sébastien
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Get full text
Journal Article
Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors
Fairhurst, Robin A., Caravatti, Giorgio, Guagnano, Vito, Aichholz, Reiner, Blanz, Joachim, Blasco, Francesca, Wipfli, Peter, Fritsch, Christine, Maira, Sauveur-Michel, Schnell, Christian, Seiler, Frank H.
Published in Bioorganic & medicinal chemistry letters (01.10.2016)
Published in Bioorganic & medicinal chemistry letters (01.10.2016)
Get full text
Journal Article
Aromatic Interactions with Phenylalanine 691 and Cysteine 828: A Concept for FMS-like Tyrosine Kinase-3 Inhibition. Application to the Discovery of a New Class of Potential Antileukemia Agents
Furet, Pascal, Bold, Guido, Meyer, Thomas, Roesel, Johannes, Guagnano, Vito
Published in Journal of medicinal chemistry (27.07.2006)
Published in Journal of medicinal chemistry (27.07.2006)
Get full text
Journal Article