Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis
Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Joncour, Agnès, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Rondet, Emilie, Peixoto, Christophe, Grassot, Jean-Marie, Picolet, Olivier, Annoot, Denis, Triballeau, Nicolas, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Blanque, Roland, Cottereaux, Celine, Vandervoort, Nele, Christophe, Thierry, Mollat, Patrick, Lamers, Marieke, Auberval, Marielle, Hrvacic, Boska, Ralic, Jovica, Oste, Line, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Deletion of a Single Allele of the Dkk1 Gene Leads to an Increase in Bone Formation and Bone Mass
Morvan, Frederic, Boulukos, Kim, Clément‐Lacroix, Philippe, Roman, Sergio Roman, Suc‐Royer, Isabelle, Vayssière, Béatrice, Ammann, Patrick, Martin, Patrick, Pinho, Sonia, Pognonec, Philippe, Mollat, Patrick, Niehrs, Christof, Baron, Roland, Rawadi, Georges
Published in Journal of bone and mineral research (01.06.2006)
Published in Journal of bone and mineral research (01.06.2006)
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The hedgehog receptor patched is involved in cholesterol transport
Bidet, Michel, Joubert, Olivier, Lacombe, Benoit, Ciantar, Marine, Nehmé, Rony, Mollat, Patrick, Brétillon, Lionel, Faure, Hélène, Bittman, Robert, Ruat, Martial, Mus-Veteau, Isabelle
Published in PloS one (08.09.2011)
Published in PloS one (08.09.2011)
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Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2‑a]pyridine Series of Autotaxin Inhibitors
Joncour, Agnès, Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Peixoto, Christophe, Annoot, Denis, Lepissier, Luce, Heiermann, Jörg, Hengeveld, Willem Jan, Pilzak, Gregor, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Galien, René, David, Christelle, Vandervoort, Nele, Christophe, Thierry, Conrath, Katja, Jans, Mia, Wohlkonig, Alexandre, Soror, Sameh, Steyaert, Jan, Touitou, Robert, Fleury, Damien, Vercheval, Lionel, Mollat, Patrick, Triballeau, Nicolas, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (14.09.2017)
Published in Journal of medicinal chemistry (14.09.2017)
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Discovery of Diarylhydantoins as New Selective Androgen Receptor Modulators
Nique, François, Hebbe, Séverine, Peixoto, Christophe, Annoot, Denis, Lefrançois, Jean-Michel, Duval, Eric, Michoux, Laurence, Triballeau, Nicolas, Lemoullec, Jean-Michel, Mollat, Patrick, Thauvin, Maxime, Prangé, Thierry, Minet, Dominique, Clément-Lacroix, Philippe, Robin-Jagerschmidt, Catherine, Fleury, Damien, Guédin, Denis, Deprez, Pierre
Published in Journal of medicinal chemistry (11.10.2012)
Published in Journal of medicinal chemistry (11.10.2012)
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Functional studies of membrane-bound and purified human Hedgehog receptor Patched expressed in yeast
Joubert, Olivier, Nehmé, Rony, Fleury, Damien, De Rivoyre, Matthieu, Bidet, Michel, Polidori, Ange, Ruat, Martial, Pucci, Bernard, Mollat, Patrick, Mus-Veteau, Isabelle
Published in Biochimica et biophysica acta (01.09.2009)
Published in Biochimica et biophysica acta (01.09.2009)
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Expression, purification and characterization of murine Dkk1 protein
Fleury, Damien, Gillard, Corinne, Lebhar, Helène, Vayssière, Béatrice, Touitou, Robert, Rawadi, Georges, Mollat, Patrick
Published in Protein expression and purification (01.07.2008)
Published in Protein expression and purification (01.07.2008)
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Differential roles of JNK and Smad2 signaling pathways in the inhibition of c-Myc-induced cell death by TGF-β
MAZARS, A, TOURNIGAND, C, MOLLAT, P, PRUNIER, C, FERRAND, N, BOURGEADE, M.-F, GESPACH, C, ATFI, A
Published in Oncogene (02.03.2000)
Published in Oncogene (02.03.2000)
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Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS‑5 Inhibitor for the Treatment of Osteoarthritis
Brebion, Franck, Gosmini, Romain, Deprez, Pierre, Varin, Marie, Peixoto, Christophe, Alvey, Luke, Jary, Hélène, Bienvenu, Natacha, Triballeau, Nicolas, Blanque, Roland, Cottereaux, Céline, Christophe, Thierry, Vandervoort, Nele, Mollat, Patrick, Touitou, Robert, Leonard, Philip, Ceuninck, Frédéric De, Botez, Iuliana, Monjardet, Alain, van der Aar, Ellen, Amantini, David
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
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Pharmacological Inhibition of the Skeletal IKKβ Reduces Breast Cancer-Induced Osteolysis
Marino, Silvia, Bishop, Ryan T., Mollat, Patrick, Idris, Aymen I.
Published in Calcified tissue international (01.08.2018)
Published in Calcified tissue international (01.08.2018)
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Anti-inflammatory, but not osteoprotective, effect of the TRAF6/CD40 inhibitor 6877002 in rodent models of local and systemic osteolysis
Marino, Silvia, Hannemann, Nicole, Bishop, Ryan T., Zeng, Feier, Carrasco, Giovana, Meurisse, Sandrine, Li, Boya, Sophocleous, Antonia, Sparatore, Anna, Baeuerle, Tobias, Vukicevic, Slobodan, Auberval, Marielle, Mollat, Patrick, Bozec, Aline, Idris, Aymen I.
Published in Biochemical pharmacology (01.01.2022)
Published in Biochemical pharmacology (01.01.2022)
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Combined administration of a small-molecule inhibitor of TRAF6 and Docetaxel reduces breast cancer skeletal metastasis and osteolysis
Bishop, Ryan T., Marino, Silvia, Carrasco, Giovana, Li, Boya, Allen, Richard J., Sparatore, Anna, Ottewell, Penelope D., Mollat, Patrick, Sims, Andrew H., Capulli, Mattia, Wang, Ning, Idris, Aymen I.
Published in Cancer letters (28.09.2020)
Published in Cancer letters (28.09.2020)
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Optimization of Selectivity and Pharmacokinetic Properties of Salt‑Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312
Temal-Laib, Taouès, Peixoto, Christophe, Desroy, Nicolas, De Lemos, Elsa, Bonnaterre, Florence, Bienvenu, Natacha, Picolet, Olivier, Sartori, Eric, Bucher, Denis, López-Ramos, Miriam, Roca Magadán, Carlos, Laenen, Wendy, Flower, Thomas, Mollat, Patrick, Bugaud, Olivier, Touitou, Robert, Pereira Fernandes, Anna, Lavazais, Stephanie, Monjardet, Alain, Borgonovi, Monica, Gosmini, Romain, Brys, Reginald, Amantini, David, De Vos, Steve, Andrews, Martin
Published in Journal of medicinal chemistry (11.01.2024)
Published in Journal of medicinal chemistry (11.01.2024)
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Identification of small molecule inhibitors of RANKL and TNF signalling as anti-inflammatory and antiresorptive agents in mice
Coste, Emmanuel, Greig, Iain R, Mollat, Patrick, Rose, Lorraine, Gray, Mohini, Ralston, Stuart H, van ‘t Hof, Rob J
Published in Annals of the rheumatic diseases (01.01.2015)
Published in Annals of the rheumatic diseases (01.01.2015)
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A TNF receptor loop peptide mimic blocks RANK ligand-induced signaling, bone resorption, and bone loss
Aoki, Kazuhiro, Saito, Hiroaki, Itzstein, Cecile, Ishiguro, Masaji, Shibata, Tatsuya, Blanque, Roland, Mian, Anower Hussain, Takahashi, Mariko, Suzuki, Yoshifumi, Yoshimatsu, Masako, Yamaguchi, Akira, Deprez, Pierre, Mollat, Patrick, Murali, Ramachandran, Ohya, Keiichi, Horne, William C, Baron, Roland
Published in The Journal of clinical investigation (01.06.2006)
Published in The Journal of clinical investigation (01.06.2006)
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Correction to Discovery, Structure–Activity Relationship, and Binding Mode of an Imidazo[1,2‑a]pyridine Series of Autotaxin Inhibitors
Joncour, Agnès, Desroy, Nicolas, Housseman, Christopher, Bock, Xavier, Bienvenu, Natacha, Cherel, Laëtitia, Labeguere, Virginie, Peixoto, Christophe, Annoot, Denis, Lepissier, Luce, Heiermann, Jörg, Hengeveld, Willem Jan, Pilzak, Gregor, Monjardet, Alain, Wakselman, Emanuelle, Roncoroni, Veronique, Le Tallec, Sandrine, Galien, René, David, Christelle, Vandervoort, Nele, Christophe, Thierry, Conrath, Katja, Jans, Mia, Wohlkonig, Alexandre, Soror, Sameh, Steyaert, Jan, Touitou, Robert, Fleury, Damien, Vercheval, Lionel, Mollat, Patrick, Triballeau, Nicolas, van der Aar, Ellen, Brys, Reginald, Heckmann, Bertrand
Published in Journal of medicinal chemistry (10.05.2018)
Published in Journal of medicinal chemistry (10.05.2018)
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Regulation of breast cancer induced bone disease by cancer-specific IKKβ
Marino, Silvia, Bishop, Ryan T, Capulli, Mattia, Sophocleous, Antonia, Logan, John G, Mollat, Patrick, Mognetti, Barbara, Ventura, Luca, Sims, Andrew H, Rucci, Nadia, Ralston, Stuart H, Idris, Aymen I
Published in Oncotarget (23.03.2018)
Published in Oncotarget (23.03.2018)
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