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6 results on '"Simonnet, Yvan"'

2. Abstract 4199: Inhibition of NF-kB inducing kinase (NIK) selectively abrogates NIK and TRAF3 mutant multiple myeloma tumor growth

Author

Versele, Matthias, primary, Janssen, Lut, additional, Geerts, Tamara, additional, Floren, Wim, additional, Janssens, Boudewijn, additional, Millar, Hillary, additional, Jacoby, Edgar, additional, Gross, Gerhard, additional, Ligny, Yannick, additional, Simonnet, Yvan, additional, Amblard, Nathalie, additional, Querolle, Olivier, additional, Csoka, Imre, additional, Poncelet, Virginie, additional, Tronel, Virginie, additional, Nocquet-Thibault, Sophie, additional, Meerpoel, Lieven, additional, Edwards, James, additional, Salvati, Marc, additional, Balasubramanian, Sriram, additional, Lenox, Laurie, additional, Theuer, Charles, additional, Attar, Ricardo, additional, and Stansfield, Ian, additional

Published
2017
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3. Abstract 3228: Characterization of a novel, orally bioavailable, potent and highly selective small molecule inhibitor of PERK: A tool to probe the biphasic concentration-dependent induction of ER stress in models of multiple myeloma and B-cell lymphoma

Author

Stansfield, Ian, primary, Ligny, Yannick, additional, Simonnet, Yvan, additional, Demestre, Christophe, additional, Amblard, Nathalie, additional, Meyer, Christophe, additional, Geerts, Tamara, additional, Ven, Jeroen Van de, additional, Wyngaert, Ilse Van den, additional, Vermeulen, Peter, additional, Beerden, Inge, additional, Peeters, Danielle, additional, Liebregts, Johnny, additional, Baelen, Kurt Van, additional, Simillion, Cedric, additional, Janssen, Boudewijn, additional, Verhulst, Tinne, additional, Esser, Norbert, additional, Bischoff, James, additional, Meerpoel, Lieven, additional, and Versele, Matthias, additional

Published
2014
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4. Abstract 4748: Discovery of JNJ-42756493, a potent fibroblast growth factor receptor (FGFR) inhibitor using a fragment based approach

Author

Angibaud, Patrick R., primary, Mevellec, Laurence, additional, Saxty, Gordon, additional, Adelinet, Christophe, additional, Akkari, Rhalid, additional, Berdini, Valerio, additional, Bonnet, Pascal, additional, Bourgeois, Marine, additional, Bourdrez, Xavier, additional, Cleasby, Anne, additional, Colombel, Helene, additional, Csoka, Imre, additional, Embrechts, Werner, additional, Freyne, Eddy, additional, Gilissen, Ronaldus, additional, Jovcheva, Eleonora, additional, King, Peter, additional, Lacrampe, Jean, additional, Lardeau, Delphine, additional, Ligny, Yannick, additional, Mcclue, Steve, additional, Meerpoel, Lieven, additional, Newell, David R., additional, Page, Martin, additional, Papanikos, Alexandra, additional, Pasquier, Elisabeth, additional, Pilatte, Isabelle, additional, Poncelet, Virginie, additional, Querolle, Olivier, additional, Rees, David C., additional, Rich, Sharna, additional, Roux, Bruno, additional, Sement, Elodie, additional, Simonnet, Yvan, additional, Squires, Matthew, additional, Tronel, Virginie, additional, Verhulst, Tinne, additional, Vialard, Jorge, additional, Willems, Marc, additional, Woodhead, Steven J., additional, Wroblowski, Berthold, additional, Murray, Christopher W., additional, and Perera, Timothy, additional

Published
2014
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5. Synthesis, Structure−Activity Relationship, and Receptor Pharmacology of a New Series of Quinoline Derivatives Acting as Selective, Noncompetitive mGlu1 Antagonists

Author

Mabire, Dominique, primary, Coupa, Sophie, additional, Adelinet, Christophe, additional, Poncelet, Alain, additional, Simonnet, Yvan, additional, Venet, Marc, additional, Wouters, Ria, additional, Lesage, Anne S. J., additional, Beijsterveldt, Ludy Van, additional, and Bischoff, François, additional

Published
2005
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6. Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.

Author

Mabire D, Coupa S, Adelinet C, Poncelet A, Simonnet Y, Venet M, Wouters R, Lesage AS, Van Beijsterveldt L, and Bischoff F

Subjects
Animals, Biological Availability, CHO Cells, Calcium metabolism, Cell Line, Tumor, Cricetinae, Cricetulus, Half-Life, Humans, In Vitro Techniques, Intracellular Fluid metabolism, Microsomes, Liver metabolism, Quinolines pharmacokinetics, Quinolines pharmacology, Rats, Receptors, Metabotropic Glutamate physiology, Signal Transduction drug effects, Stereoisomerism, Structure-Activity Relationship, Quinolines chemical synthesis, Receptors, Metabotropic Glutamate antagonists & inhibitors
Abstract

We describe the discovery and the structure-activity relationship of a new series of quinoline derivatives acting as selective and highly potent noncompetitive mGlu1 antagonists. We first identified cis-10 as a fairly potent mGlu1 antagonist (IC(50) = 20 nM) in a cell-based signal transduction assay on the rat mGlu1 receptor expressed in CHO-K1 cells, and then we were able to design and synthesize highly potent compounds on both rat and human mGlu1 receptors as exemplified by compound cis-64a, which has an antagonist potency of 0.5 nM for the human mGlu1 receptor. We briefly present and discuss the in vitro metabolic stability of the compounds in human liver microsomes. We finally report the pharmacokinetic properties of our lead compound cis-64a.

Published
2005
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