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Alain De Pover
Researcher at Novartis
Publications - 21
Citations - 2730
Alain De Pover is an academic researcher from Novartis. The author has contributed to research in topics: Kinase & PI3K/AKT/mTOR pathway. The author has an hindex of 15, co-authored 21 publications receiving 2539 citations.
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Journal ArticleDOI
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
Sauveur-Michel Maira,Frédéric Stauffer,Josef Brueggen,Pascal Furet,Christian Schnell,Christine Fritsch,Saskia M. Brachmann,Patrick Chène,Alain De Pover,Kevin Schoemaker,Doriano Fabbro,Daniela Gabriel,Marjo Simonen,Leon Murphy,Peter Finan,William R. Sellers,Carlos Garcia-Echeverria +16 more
TL;DR: The preclinical data show that NVP-BEZ235 is a potent dual PI3K/mTOR modulator with favorable pharmaceutical properties, and the compound was well tolerated, displayed disease stasis when administered orally, and enhanced the efficacy of other anticancer agents when used in in vivo combination studies.
Journal ArticleDOI
Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor
Sauveur-Michel Maira,Sabina Pecchi,Alan Huang,Matthew Burger,Mark Knapp,Dario Sterker,Christian Schnell,Daniel Guthy,Tobi Nagel,Marion Wiesmann,Saskia M. Brachmann,Christine Fritsch,Marion Dorsch,Patrick Chène,Kevin Shoemaker,Alain De Pover,Daniel Menezes,Georg Martiny-Baron,Doriano Fabbro,Christine D. Wilson,Robert Schlegel,Francesco Hofmann,Carlos Garcia-Echeverria,William R. Sellers,Charles Voliva +24 more
TL;DR: The biologic characterization of the 2-morpholino pyrimidine derivative pan-PI3K inhibitor NVP-BKM120 shows dose-dependent in vivo pharmacodynamic activity as measured by significant inhibition of p-Akt and tumor growth inhibition in mechanistic xenograft models and behaves synergistically when combined with either targeted agentssuch as MEK or HER2 inhibitors or with cytotoxic agents such as docetaxel or temozolomide.
Journal ArticleDOI
Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials
Christine Fritsch,Alan Huang,Christian Chatenay-Rivauday,Christian Schnell,Anupama Reddy,Manway Liu,Audrey Kauffmann,Daniel Guthy,Dirk Erdmann,Alain De Pover,Pascal Furet,Hui Gao,Stephane Ferretti,Youzhen Wang,Joerg Trappe,Saskia M. Brachmann,Sauveur-Michel Maira,Christine D. Wilson,Markus Boehm,Carlos Garcia-Echeverria,Patrick Chène,Marion Wiesmann,Robert Cozens,Joseph Lehar,Robert Schlegel,Giorgio Caravatti,Francesco Hofmann,William R. Sellers +27 more
TL;DR: The biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selective inhibitor of PI3Kα and its most common oncogenic mutant forms, are reported and it is found that PIK3CA mutation was the foremost positive predictor of sensitivity while revealing additional positive and negative associations such as Pik3CA amplification and PTEN mutation, respectively.
Journal ArticleDOI
Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition
Oliver Weigert,Andrew A. Lane,Liat Bird,Nadja Kopp,Bjoern Chapuy,Diederik van Bodegom,Angela V. Toms,Sachie Marubayashi,Amanda L. Christie,Michael R. McKeown,Ronald M. Paranal,James E. Bradner,Akinori Yoda,Christoph Gaul,Eric Vangrevelinghe,Vincent Romanet,Masato Murakami,Ralph Tiedt,Nicolas Ebel,Emeline Evrot,Alain De Pover,Catherine H. Régnier,Dirk Erdmann,Francesco Hofmann,Michael J. Eck,Stephen E. Sallan,Ross L. Levine,Andrew L. Kung,Fabienne Baffert,Thomas Radimerski,David M. Weinstock +30 more
TL;DR: Hsp90 inhibition in B cell acute lymphoblastic leukemia overcomes resistance to JAK2 inhibitors and induces apoptotic cell death in mice treated with these inhibitors.
Journal ArticleDOI
Characterisation of Na/K-ATPase, its isoforms, and the inotropic response to ouabain in isolated failing human hearts.
Olga I. Shamraj,Ingrid L. Grupp,G. Grupp,David Melvin,Nathalie Gradoux,Walter Kremers,Jerry B. Lingrel,Alain De Pover +7 more
TL;DR: This study shows conclusively, for the first time, that failing human hearts are more sensitive to ouabain.