Search Results - "Sanière, Laurent"

Discovery and Optimization of Orally Bioavailable Phthalazone and Cinnolone Carboxylic Acid Derivatives as S1P2 Antagonists against Fibrotic Diseases by Mammoliti, Oscar, Jansen, Koen, El Bkassiny, Sandy, Palisse, Adeline, Triballeau, Nicolas, Bucher, Denis, Allart, Brigitte, Jaunet, Alex, Tricarico, Giovanni, De Wachter, Maxim, Menet, Christel, Blanc, Javier, Letfus, Vatroslav, Rupčić, Renata, Šmehil, Mario, Poljak, Tanja, Coornaert, Beatrice, Sonck, Kathleen, Duys, Inge, Waeckel, Ludovic, Lecru, Lola, Marsais, Florence, Jagerschmidt, Catherine, Auberval, Marielle, Pujuguet, Philippe, Oste, Line, Borgonovi, Monica, Wakselman, Emanuelle, Christophe, Thierry, Houvenaghel, Nicolas, Jans, Mia, Heckmann, Bertrand, Sanière, Laurent, Brys, Reginald

“…Idiopathic pulmonary fibrosis (IPF) is a chronic and progressive lung disease. Current treatments only slow down disease progression, making new therapeutic…”
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Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis by Mammoliti, Oscar, Palisse, Adeline, Joannesse, Caroline, El Bkassiny, Sandy, Allart, Brigitte, Jaunet, Alex, Menet, Christel, Coornaert, Beatrice, Sonck, Kathleen, Duys, Inge, Clément-Lacroix, Philippe, Oste, Line, Borgonovi, Monica, Wakselman, Emanuelle, Christophe, Thierry, Houvenaghel, Nicolas, Jans, Mia, Heckmann, Bertrand, Sanière, Laurent, Brys, Reginald

“…Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling could be effective for the treatment of idiopathic pulmonary…”
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Discovery of 9‑Cyclopropylethynyl-2-((S)‑1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1‑a]­isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial by Labéguère, Frédéric, Dupont, Sonia, Alvey, Luke, Soulas, Florilène, Newsome, Gregory, Tirera, Amynata, Quenehen, Vanessa, Mai, Thi Thu Trang, Deprez, Pierre, Blanqué, Roland, Oste, Line, Le Tallec, Sandrine, De Vos, Steve, Hagers, Annick, Vandevelde, Ann, Nelles, Luc, Vandervoort, Nele, Conrath, Katja, Christophe, Thierry, van der Aar, Ellen, Wakselman, Emanuelle, Merciris, Didier, Cottereaux, Céline, da Costa, Cécile, Saniere, Laurent, Clement-Lacroix, Philippe, Jenkins, Laura, Milligan, Graeme, Fletcher, Stephen, Brys, Reginald, Gosmini, Romain

“…GPR84 is a medium chain free fatty acid-binding G-protein-coupled receptor associated with inflammatory and fibrotic diseases. As the only reported antagonist…”
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Discovery and Optimization of an Azetidine Chemical Series As a Free Fatty Acid Receptor 2 (FFA2) Antagonist: From Hit to Clinic by Pizzonero, Mathieu, Dupont, Sonia, Babel, Marielle, Beaumont, Stéphane, Bienvenu, Natacha, Blanqué, Roland, Cherel, Laëtitia, Christophe, Thierry, Crescenzi, Benedetta, De Lemos, Elsa, Delerive, Philippe, Deprez, Pierre, De Vos, Steve, Djata, Fatoumata, Fletcher, Stephen, Kopiejewski, Sabrina, L’Ebraly, Christelle, Lefrançois, Jean-Michel, Lavazais, Stéphanie, Manioc, Murielle, Nelles, Luc, Oste, Line, Polancec, Denis, Quénéhen, Vanessa, Soulas, Florilène, Triballeau, Nicolas, van der Aar, Ellen M, Vandeghinste, Nick, Wakselman, Emanuelle, Brys, Reginald, Saniere, Laurent

“…FFA2, also called GPR43, is a G-protein coupled receptor for short chain fatty acids which is involved in the mediation of inflammatory responses. A class of…”
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The Medium-Chain Fatty Acid Receptor GPR84 Mediates Myeloid Cell Infiltration Promoting Steatohepatitis and Fibrosis by Puengel, Tobias, De Vos, Steve, Hundertmark, Jana, Kohlhepp, Marlene, Guldiken, Nurdan, Pujuguet, Philippe, Auberval, Marielle, Marsais, Florence, Shoji, Kenji F, Saniere, Laurent, Trautwein, Christian, Luedde, Tom, Strnad, Pavel, Brys, Reginald, Clément-Lacroix, Philippe, Tacke, Frank

“…Medium-chain fatty acids (MCFAs) have been associated with anti-steatotic effects in hepatocytes. Expression of the MCFA receptor GPR84 (G protein-coupled…”
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Pharmacological targeting of the ephrin receptor kinase signalling by GLPG1790 in vitro and in vivo reverts oncophenotype, induces myogenic differentiation and radiosensitizes embryonal rhabdomyosarcoma cells by Megiorni, Francesca, Gravina, Giovanni Luca, Camero, Simona, Ceccarelli, Simona, Del Fattore, Andrea, Desiderio, Vincenzo, Papaccio, Federica, McDowell, Heather P, Shukla, Rajeev, Pizzuti, Antonio, Beirinckx, Filip, Pujuguet, Philippe, Saniere, Laurent, der Aar, Ellen Van, Maggio, Roberto, De Felice, Francesca, Marchese, Cinzia, Dominici, Carlo, Tombolini, Vincenzo, Festuccia, Claudio, Marampon, Francesco

“…EPH (erythropoietin-producing hepatocellular) receptors are clinically relevant targets in several malignancies. This report describes the effects of GLPG1790,…”
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Reinvestigation of the Branimycin Stereochemistry at Position 17‑C by Čikoš, Ana, Triballeau, Nicolas, Hubbard, Paul A, Žiher, Dinko, Stouten, Pieter F. W, Doyon, Julien G. P.-O, Deschrijver, Tiny, Wouters, Johan, Lépine, Renaud H. M, Saniere, Laurent

“…A conformational study of branimycin was performed using single-crystal X-ray crystallography to characterize the solid-state form, while a combination of NMR…”
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Novel Approaches to Optically Active Substituted 4,5-Dihydro-1,2,4-triazin-6(1H)-ones as Conformationally Constrained Peptidomimetics by Bourguignon, Jean-Jacques, Saniere, Laurènt, Schmitt, Martine, Pellegrini, Nadia

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Copper-Catalyzed Nitrogen Transfer Mediated by Iodosylbenzene PhIO by Dauban, Philippe, Sanière, Laurent, Tarrade, Aurélie, Dodd, Robert H

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Mo1234 The FFA2 Antagonist GLPG0974: A Promising Approach to Treat Neutrophil-Driven Inflammation by Vanhoutte, Frédéric P, Namour, Florence S, Dupont, Sonia, Pizzonero, Mathieu, De Vos, Steve, Sanière, Laurent, van der Aa, Annegret, Beetens, Johan, van 't Klooster, Gerben

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Iminoiodane mediated aziridination of α-allylglycine: access to a novel rigid arginine derivative and to the natural amino acid enduracididine by Sanière, Laurent, Leman, Loı̈c, Bourguignon, Jean-Jacques, Dauban, Philippe, Dodd, Robert H

“…The synthesis of fully protected aminodihydrohistidines in optically pure form is described starting from allylglycine derivatives. These compounds represent…”
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Copper-catalyzed aziridination of allylglycine derivatives by Leman, Loic, Saniere, Laurent, Dauban, Philippe, Dodd, Robert H.

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Ex vivo tissue perturbations coupled to single-cell RNA-seq reveal multilineage cell circuit dynamics in human lung fibrogenesis by Lang, Niklas J, Gote-Schniering, Janine, Porras-Gonzalez, Diana, Yang, Lin, De Sadeleer, Laurens J, Jentzsch, R Christoph, Shitov, Vladimir A, Zhou, Shuhong, Ansari, Meshal, Agami, Ahmed, Mayr, Christoph H, Hooshiar Kashani, Baharak, Chen, Yuexin, Heumos, Lukas, Pestoni, Jeanine C, Molnar, Eszter Sarolta, Geeraerts, Emiel, Anquetil, Vincent, Saniere, Laurent, Wögrath, Melanie, Gerckens, Michael, Lehmann, Mareike, Yildirim, Ali Önder, Hatz, Rudolf, Kneidinger, Nikolaus, Behr, Jürgen, Wuyts, Wim A, Stoleriu, Mircea-Gabriel, Luecken, Malte D, Theis, Fabian J, Burgstaller, Gerald, Schiller, Herbert B

“…Pulmonary fibrosis develops as a consequence of failed regeneration after injury. Analyzing mechanisms of regeneration and fibrogenesis directly in human…”
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The Small Molecule Ephrin Receptor Inhibitor, GLPG1790, Reduces Renewal Capabilities of Cancer Stem Cells, Showing Anti-Tumour Efficacy on Preclinical Glioblastoma Models by Gravina, Giovanni Luca, Mancini, Andrea, Colapietro, Alessandro, Delle Monache, Simona, Sferra, Roberta, Vitale, Flora, Cristiano, Loredana, Martellucci, Stefano, Marampon, Francesco, Mattei, Vincenzo, Beirinckx, Filip, Pujuguet, Philippe, Saniere, Laurent, Lorenzon, Giocondo, van der Aar, Ellen, Festuccia, Claudio

“…Therapies against glioblastoma (GBM) show a high percentage of failure associated with the survival of glioma stem cells (GSCs) that repopulate treated…”
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Copper-Catalyzed Nitrogen Transfer Mediated by Iodosylbenzene PhIO by Dauban, Philippe, Sanière, Laurent, Tarrade, Aurélie, Dodd, Robert H.

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Antitumorigenic Effects of Inhibiting Ephrin Receptor Kinase Signaling by GLPG1790 against Colorectal Cancer Cell Lines In Vitro and In Vivo by Van der Aar, Ellen, Musio, Daniela, Mattei, Vincenzo, Martellucci, Stefano, Maggio, Roberto, Tombolini, Vincenzo, Festuccia, Claudio, Marampon, Francesco, Saniere, Laurent, Pujuguet, Philippe, Beirinckx, Filip, Scicchitano, Bianca Maria, Fasciani, Irene, Petragnano, Francesco, Gravina, Giovanni Luca, Colapietro, Alessandro, De Felice, Francesca

“…Erythropoietin-producing hepatocellular receptors (Eph) promote the onset and sustain the progression of cancers such as colorectal cancer (CRC), in which the…”
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Abstract 1753: GLPG1790: The first Ephrin (EPH) receptor tyrosine kinase inhibitor for the treatment of triple negative breast cancer by Pujuguet, Philippe, Beirinckx, Filip, Delachaume, Carole, Huck, Jacques, Aar, Ellen Van der, Brys, Reginald, Rompaey, Luc Van, Wigerinck, Piet, Saniere, Laurent

“…Abstract Receptor tyrosine kinases define a clinically relevant class of targets in the field of cancer. Here we report the discovery of a pre-clinical drug…”
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Regioselective alkylations of optically active 4,5-dihydro-1,2,4-triazin-6(1 H)-ones by Sanière, Laurent, Schmitt, Martine, Bourguignon, Jean-Jacques

“…Regiocontrolled alkylations of chiral 4,5-dihydrotriazin-6-ones using sodium hydride in DMF are reported. By this approach different N1-alkyl, N1,N4-dialkyl…”
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Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors by Rankovic, Zoran, Cai, Jiaqiang, Kerr, Jennifer, Fradera, Xavier, Robinson, John, Mistry, Ashvin, Hamilton, Emma, McGarry, George, Andrews, Fiona, Caulfield, Wilson, Cumming, Iain, Dempster, Maureen, Waller, John, Scullion, Paul, Martin, Iain, Mitchell, Ann, Long, Clive, Baugh, Mark, Westwood, Paul, Kinghorn, Emma, Bruin, John, Hamilton, William, Uitdehaag, Joost, Zeeland, Mario van, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, François, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric

“…Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with improved pharmacokinetic…”
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2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors by Cai, Jiaqiang, Bennett, D. Jonathan, Rankovic, Zoran, Dempster, Maureen, Fradera, Xavier, Gillespie, Jonathan, Cumming, Iain, Finlay, William, Baugh, Mark, Boucharens, Sylviane, Bruin, John, Cameron, Kenneth S., Hamilton, William, Kerr, Jennifer, Kinghorn, Emma, McGarry, George, Robinson, John, Scullion, Paul, Uitdehaag, Joost C.M., van Zeeland, Mario, Potin, Dominique, Saniere, Laurent, Fouquet, Andre, Chevallier, Francois, Deronzier, Hortense, Dorleans, Cecile, Nicolai, Eric

“…2-Phenyl-9H-purine-6-carbonitrile derivatives were designed as selective human cathepsin S inhibitors through P2 optimization and transition state…”
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