المؤلفون: Taouès Temal-Laib, Christophe Peixoto, Nicolas Desroy, Elsa De Lemos, Florence Bonnaterre, Natacha Bienvenu, Olivier Picolet, Eric Sartori, Denis Bucher, Miriam López-Ramos, Carlos Roca Magadán, Wendy Laenen, Thomas Flower, Patrick Mollat, Olivier Bugaud, Robert Touitou, Anna Pereira Fernandes, Stephanie Lavazais, Alain Monjardet, Monica Borgonovi, Romain Gosmini, Reginald Brys, David Amantini, Steve De Vos, Martin Andrews

مصطلحات موضوعية: Biochemistry, Cell Biology, Genetics, Molecular Biology, Pharmacology, Immunology, Cancer, Inorganic Chemistry, Hematology, Infectious Diseases, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, throughput screening campaign, protein kinase amp, activated protein kinase, immunoregulatory cytokine production, clinical candidate glpg3312, pharmacokinetic investigations led, pharmacokinetic properties, immunoregulatory activities, glpg3312 demonstrated, vivo <, vitro <, threonine kinases, therapeutic potential, subsequent hit, sik inhibitor, mouse models, inducible kinases, dual mechanism

العلاقة: https://figshare.com/articles/journal_contribution/Optimization_of_Selectivity_and_Pharmacokinetic_Properties_of_Salt_Inducible_Kinase_Inhibitors_that_Led_to_the_Discovery_of_Pan-SIK_Inhibitor_GLPG3312/24904973Test

الإتاحة: https://doi.org/10.1021/acs.jmedchem.3c01428.s001Test
https://figshare.com/articles/journal_contribution/Optimization_of_Selectivity_and_Pharmacokinetic_Properties_of_Salt_Inducible_Kinase_Inhibitors_that_Led_to_the_Discovery_of_Pan-SIK_Inhibitor_GLPG3312/24904973Test

المؤلفون: Franck Brebion (2439052), Romain Gosmini (1738168), Pierre Deprez (1705699), Marie Varin (2479900), Christophe Peixoto (2035117), Luke Alvey (2035129), Hélène Jary (2035114), Natacha Bienvenu (1705657), Nicolas Triballeau (1400671), Roland Blanque (3989681), Céline Cottereaux (9412031), Thierry Christophe (242276), Nele Vandervoort (3989705), Patrick Mollat (206614), Robert Touitou (4376779), Philip Leonard (1621432), Frédéric De Ceuninck (1417306), Iuliana Botez (1701322), Alain Monjardet (3989687), Ellen van der Aar (3989690), David Amantini (232220)

مصطلحات موضوعية: Biochemistry, Medicine, Cell Biology, Neuroscience, Physiology, Pharmacology, Biotechnology, Cancer, Science Policy, Infectious Diseases, Biological Sciences not elsewhere classified, Chemical Sciences not elsewhere classified, phase 2, knee OA, 1.5 μ M, DMOAD, hydantoin series, Biochemical activity, cocrystal structure, anticatabolic activity, IC 50, glycosaminoglycan release, disease-modifying osteoarthritis, mouse cartilage explants, NCT, GLPG, aggrecanase ADAMTS, HTS, fluorescence-based assay, AGC ELISA

العلاقة: https://figshare.com/articles/journal_contribution/Discovery_of_GLPG1972_S201086_a_Potent_Selective_and_Orally_Bioavailable_ADAMTS_5_Inhibitor_for_the_Treatment_of_Osteoarthritis/14217024Test

الإتاحة: https://doi.org/10.1021/acs.jmedchem.0c02008.s001Test

المؤلفون: Alain Monjardet, Thierry Christophe, Nicolas Triballeau, Helene Jary, Luke Jonathan Alvey, Romain Luc Marie Gosmini, Frédéric André De Ceuninck, Pierre Deprez, Robert Touitou, Roland Blanque, D. Amantini, Nele Vandervoort, Ellen van der Aar, Philip Leonard, F. Brebion, Patrick Mollat, Natacha Bienvenu, C. Cottereaux, I. Botez, Varin Marie Laurence Claire, Christophe Peixoto

المصدر: Journal of Medicinal Chemistry. 64:2937-2952

مصطلحات موضوعية: Cartilage, Articular, Models, Molecular, Osteoarthritis, Pharmacology, 01 natural sciences, law.invention, Glycosaminoglycan, Mice, 03 medical and health sciences, Dogs, law, Drug Discovery, medicine, Animals, Humans, IC50, Aggrecan, Glycosaminoglycans, 030304 developmental biology, Aggrecanase, 0303 health sciences, Chemistry, Cartilage, ADAMTS, medicine.disease, Rats, 0104 chemical sciences, Mice, Inbred C57BL, 010404 medicinal & biomolecular chemistry, medicine.anatomical_structure, Recombinant DNA, Molecular Medicine, ADAMTS5 Protein

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e63e1d09bcd2c3ffc719892459e89ab3Test
https://doi.org/10.1021/acs.jmedchem.0c02008Test

المؤلفون: Christelle David, Nele Vandervoort, Damien Fleury, Denis Annoot, Laëtitia Cherel, Willem Jan Hengeveld, Thierry Christophe, Sameh H. Soror, Agnès Marie Joncour, Christopher Gaëtan Housseman, Alain Monjardet, R Galien, Patrick Mollat, Reginald Brys, Veronique Roncoroni, Luce Lepissier, Natacha Bienvenu, Lionel Vercheval, Alexandre Wohlkonig, Christophe Peixoto, Jörg Heiermann, Katja Conrath, Mia Jans, Sandrine Le Tallec, Bertrand Heckmann, Robert Touitou, Nicolas Desroy, Jan Steyaert, Virginie Labeguere, Gregor Pilzak, Ellen van der Aar, Xavier Marie Bock, Nicolas Triballeau, Emanuelle Wakselman

المساهمون: Department of Bio-engineering Sciences, Structural Biology Brussels

المصدر: Journal of Medicinal Chemistry. 60:7371-7392

مصطلحات موضوعية: Male, 0301 basic medicine, Phosphodiesterase Inhibitors, Pyridines, Stereochemistry, Inflammation, 01 natural sciences, Cocrystal, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Drug Discovery, Lysophosphatidic acid, Hydrolase, medicine, Animals, Humans, Structure–activity relationship, chemistry.chemical_classification, Phosphoric Diester Hydrolases, 010405 organic chemistry, Chemistry, Drug discovery, Imidazoles, Lysophosphatidylcholines, Rats, 0104 chemical sciences, Molecular Docking Simulation, 030104 developmental biology, Enzyme, Biochemistry, Molecular Medicine, lipids (amino acids, peptides, and proteins), Lysophospholipids, Autotaxin, medicine.symptom

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1bab957aedfbab6da364d90d0e33f16Test
https://doi.org/10.1021/acs.jmedchem.7b00647Test

المؤلفون: Elsa De Lemos, Vanessa Quenehen, Laëtitia Cherel, Nicolas Triballeau, Reginald Brys, Stéphane Beaumont, Florilène Soulas, Murielle Manioc, Thierry Christophe, Emanuelle Wakselman, Ellen van der Aar, Natacha Bienvenu, Christelle L’Ebraly, Luc Nelles, Line Oste, Laurent Saniere, Fatoumata Djata, Stéphanie Lavazais, Philippe Delerive, Stephen Robert Fletcher, Steve De Vos, Mathieu Rafaël Pizzonero, Sabrina Kopiejewski, S. Dupont, Nick Vandeghinste, Jean-Michel Lefrancois, Benedetta Crescenzi, Denis Polancec, Marielle Babel, Pierre Deprez, Roland Blanque

المصدر: Journal of Medicinal Chemistry. 57:10044-10057

مصطلحات موضوعية: Azetidine, Receptors, Cell Surface, Thiophenes, Pharmacology, Rats, Sprague-Dawley, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Drug Discovery, Free fatty acid receptor 2, Animals, Humans, Potency, Structure–activity relationship, Leukocyte disorder, Receptor, ADME, Chemistry, Anti-Inflammatory Agents, Non-Steroidal, Antagonist, Butyrates, Immune System Diseases, Biochemistry, Microsomes, Liver, Azetidines, Molecular Medicine, Leukocyte Disorders

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33097c7d0222ebea1a74983132fa64b7Test
https://doi.org/10.1021/jm5012885Test

المؤلفون: Nele Vandervoort, Xavier Marie Bock, Patrick Mollat, Jovica Ralić, Alain Monjardet, Nicolas Triballeau, Thierry Christophe, Ellen van der Aar, Marieke Lamers, Boska Hrvacic, Nicolas Desroy, Bertrand Heckmann, Line Oste, Emilie Rondet, Virginie Labeguere, Roland Blanque, Veronique Roncoroni, Christopher Gaëtan Housseman, Sandrine Le Tallec, Natacha Bienvenu, C. Cottereaux, M. Auberval, Reginald Brys, Laëtitia Cherel, Emanuelle Wakselman, Picolet Olivier Laurent, Jean-Marie Grassot, Agnès Marie Joncour, Christophe Peixoto, Denis Annoot

مصطلحات موضوعية: 0301 basic medicine, hERG, Pharmacology, autoaxin inhibitor, LPA, pulmonary fibrosis, bleomycin-induced model in mice, 03 medical and health sciences, Idiopathic pulmonary fibrosis, chemistry.chemical_compound, Mice, 0302 clinical medicine, In vivo, Drug Discovery, Pulmonary fibrosis, medicine, Animals, Humans, Thiazole, Mice, Knockout, Lung, medicine.diagnostic_test, biology, Chemistry, Phosphoric Diester Hydrolases, Imidazoles, medicine.disease, Idiopathic Pulmonary Fibrosis, Rats, 030104 developmental biology, Bronchoalveolar lavage, medicine.anatomical_structure, Pyrimidines, 030220 oncology & carcinogenesis, biology.protein, Molecular Medicine, lipids (amino acids, peptides, and proteins), Autotaxin

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04c6f6e80895c7ca93e77aad9243c383Test
https://www.bib.irb.hr/981523Test

المؤلفون: Reginald Brys, Emanuelle Wakselman, Lionel Vercheval, Christelle David, Nele Vandervoort, Laëtitia Cherel, Christopher Gaëtan Housseman, Luce Lepissier, Natacha Bienvenu, Mia Jans, Alain Monjardet, Agnès Marie Joncour, Nicolas Desroy, Gregor Pilzak, Willem Jan Hengeveld, Sandrine Le Tallec, Ellen van der Aar, Bertrand Heckmann, Nicolas Triballeau, Jan Steyaert, Patrick Mollat, Veronique Roncoroni, Virginie Labeguere, Sameh H. Soror, Damien Fleury, Thierry Christophe, Christophe Peixoto, Xavier Marie Bock, Denis Annoot, Jörg Heiermann, Katja Conrath, R Galien, Robert Touitou, Alexandre Wohlkonig

المصدر: Journal of Medicinal Chemistry. 61:4270-4270

مصطلحات موضوعية: chemistry.chemical_compound, Series (mathematics), chemistry, Stereochemistry, Drug Discovery, Pyridine, Molecular Medicine, Structure–activity relationship, Autotaxin

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93dee812f5866eca6cabf47d605a46ceTest
https://doi.org/10.1021/acs.jmedchem.8b00579Test