Discovery of Epigenetic Regulator I‑BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
Mirguet, Olivier, Gosmini, Romain, Toum, Jérôme, Clément, Catherine A, Barnathan, Mélanie, Brusq, Jean-Marie, Mordaunt, Jacqueline E, Grimes, Richard M, Crowe, Miriam, Pineau, Olivier, Ajakane, Myriam, Daugan, Alain, Jeffrey, Phillip, Cutler, Leanne, Haynes, Andrea C, Smithers, Nicholas N, Chung, Chun-wa, Bamborough, Paul, Uings, Iain J, Lewis, Antonia, Witherington, Jason, Parr, Nigel, Prinjha, Rab K, Nicodème, Edwige
Published in Journal of medicinal chemistry (10.10.2013)
Published in Journal of medicinal chemistry (10.10.2013)
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The Discovery of I‑BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor
Gosmini, Romain, Nguyen, Van Loc, Toum, Jérôme, Simon, Christophe, Brusq, Jean-Marie G, Krysa, Gael, Mirguet, Olivier, Riou-Eymard, Alizon M, Boursier, Eric V, Trottet, Lionel, Bamborough, Paul, Clark, Hugh, Chung, Chun-wa, Cutler, Leanne, Demont, Emmanuel H, Kaur, Rejbinder, Lewis, Antonia J, Schilling, Mark B, Soden, Peter E, Taylor, Simon, Walker, Ann L, Walker, Matthew D, Prinjha, Rab K, Nicodème, Edwige
Published in Journal of medicinal chemistry (09.10.2014)
Published in Journal of medicinal chemistry (09.10.2014)
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A new AMPK activator, GSK773, corrects fatty acid oxidation and differentiation defect in CPT2-deficient myotubes
Boufroura, Fatima-Zohra, Le Bachelier, Carole, Tomkiewicz-Raulet, Céline, Schlemmer, Dimitri, Benoist, Jean-François, Grondin, Pascal, Lamotte, Yann, Mirguet, Olivier, Mouillet-Richard, Sophie, Bastin, Jean, Djouadi, Fatima
Published in Human molecular genetics (01.10.2018)
Published in Human molecular genetics (01.10.2018)
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Journal Article
From ApoA1 upregulation to BET family bromodomain inhibition: Discovery of I-BET151
Mirguet, Olivier, Lamotte, Yann, Donche, Frédéric, Toum, Jérôme, Gellibert, Françoise, Bouillot, Anne, Gosmini, Romain, Nguyen, Van-Loc, Delannée, Delphine, Seal, Jonathan, Blandel, Florence, Boullay, Anne-Bénédicte, Boursier, Eric, Martin, Sandrine, Brusq, Jean-Marie, Krysa, Gael, Riou, Alizon, Tellier, Rémi, Costaz, Agnès, Huet, Pascal, Dudit, Yann, Trottet, Lionel, Kirilovsky, Jorge, Nicodeme, Edwige
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
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Abstract 4501: First reported PIM kinase degraders: Design, profiling & optimization
Legros, Celine, Ratcliffe, Paul, Porkolab, Vanessa, Modugno, Michele, Mirguet, Olivier
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
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Journal Article
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia
Dawson, Mark A., Prinjha, Rab K., Dittmann, Antje, Giotopoulos, George, Bantscheff, Marcus, Chan, Wai-In, Robson, Samuel C., Chung, Chun-wa, Hopf, Carsten, Savitski, Mikhail M., Huthmacher, Carola, Gudgin, Emma, Lugo, Dave, Beinke, Soren, Chapman, Trevor D., Roberts, Emma J., Soden, Peter E., Auger, Kurt R., Mirguet, Olivier, Doehner, Konstanze, Delwel, Ruud, Burnett, Alan K., Jeffrey, Phillip, Drewes, Gerard, Lee, Kevin, Huntly, Brian J. P., Kouzarides, Tony
Published in Nature (London) (27.10.2011)
Published in Nature (London) (27.10.2011)
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Targeting non-alcoholic fatty liver disease: Design, X-ray co-crystal structure and synthesis of ‘first-in-kind’ inhibitors of serine/threonine kinase25
Kiyeleko, Scarlett, Hocine, Sofiane, Mautino, Giséle, Kuenemann, Mélaine, Nawrotek, Agata, Miallau, Linda, Vuillard, Laurent-Michel, Mirguet, Olivier, Kotschy, Andras, Hanessian, Stephen
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
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Journal Article
Discovery and Characterizatlion of Small Molecule Inhibitors of the BET Family Bromodomains
Chung, Chun-wa, Coste, Herve, White, Julia H., Mirguet, Olivier, Wilde, Jonathan, Gosmini, Romain L., Delves, Chris, Magny, Sylvie M., Woodward, Robert, Hughes, Stephen A., Boursier, Eric V., Flynn, Helen, Bouillot, Anne M., Bamborough, Paul, Brusq, Jean-Marie G., Gellibert, Francoise J., Jones, Emma J., Riou, Alizon M., Homes, Paul, Martin, Sandrine L., Uings, Iain J., Toum, Jerome, Clement, Catherine A., Boullay, Anne-Benedicte, Grimley, Rachel L., Blande, Florence M., Prinjha, Rab K., Lee, Kevin, Kirilovsky, Jorge, Nicodeme, Edwige
Published in Journal of medicinal chemistry (09.06.2011)
Published in Journal of medicinal chemistry (09.06.2011)
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Deep generative models for ligand‐based de novo design applied to multi‐parametric optimization
Perron, Quentin, Mirguet, Olivier, Tajmouati, Hamza, Skiredj, Adam, Rojas, Anne, Gohier, Arnaud, Ducrot, Pierre, Bourguignon, Marie‐Pierre, Sansilvestri‐Morel, Patricia, Do Huu, Nicolas, Gellibert, Françoise, Gaston‐Mathé, Yann
Published in Journal of computational chemistry (15.04.2022)
Published in Journal of computational chemistry (15.04.2022)
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Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis
Mole, Damian J, Webster, Scott P, Uings, Iain, Zheng, Xiaozhong, Binnie, Margaret, Wilson, Kris, Hutchinson, Jonathan P, Mirguet, Olivier, Walker, Ann, Beaufils, Benjamin, Ancellin, Nicolas, Trottet, Lionel, Bénéton, Véronique, Mowat, Christopher G, Wilkinson, Martin, Rowland, Paul, Haslam, Carl, McBride, Andrew, Homer, Natalie Z M, Baily, James E, Sharp, Matthew G F, Garden, O James, Hughes, Jeremy, Howie, Sarah E M, Holmes, Duncan S, Liddle, John, Iredale, John P
Published in Nature medicine (01.02.2016)
Published in Nature medicine (01.02.2016)
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Journal Article
Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)
Seal, Jonathan, Lamotte, Yann, Donche, Frédéric, Bouillot, Anne, Mirguet, Olivier, Gellibert, Françoise, Nicodeme, Edwige, Krysa, Gael, Kirilovsky, Jorge, Beinke, Soren, McCleary, Scott, Rioja, Inma, Bamborough, Paul, Chung, Chun-Wa, Gordon, Laurie, Lewis, Toni, Walker, Ann L., Cutler, Leanne, Lugo, David, Wilson, David M., Witherington, Jason, Lee, Kevin, Prinjha, Rab K.
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
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Journal Article
Discovery and Characterization of Small Molecule Inhibitors of the BET Family Bromodomains
Chung, Chun-wa, Coste, Hervé, White, Julia H, Mirguet, Olivier, Wilde, Jonathan, Gosmini, Romain L, Delves, Chris, Magny, Sylvie M, Woodward, Robert, Hughes, Stephen A, Boursier, Eric V, Flynn, Helen, Bouillot, Anne M, Bamborough, Paul, Brusq, Jean-Marie G, Gellibert, Françoise J, Jones, Emma J, Riou, Alizon M, Homes, Paul, Martin, Sandrine L, Uings, Iain J, Toum, Jérôme, Clément, Catherine A, Boullay, Anne-Bénédicte, Grimley, Rachel L, Blandel, Florence M, Prinjha, Rab K, Lee, Kevin, Kirilovsky, Jorge, Nicodeme, Edwige
Published in Journal of medicinal chemistry (09.06.2011)
Published in Journal of medicinal chemistry (09.06.2011)
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Journal Article
A Diverted Total Synthesis of Mycolactone Analogues: An Insight into Buruli Ulcer Toxins
Chany, Anne-Caroline, Casarotto, Virginie, Schmitt, Marjorie, Tarnus, Céline, Guenin-Macé, Laure, Demangel, Caroline, Mirguet, Olivier, Eustache, Jacques, Blanchard, Nicolas
Published in Chemistry : a European journal (16.12.2011)
Published in Chemistry : a European journal (16.12.2011)
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Journal Article
Development of a Series of Kynurenine 3‑Monooxygenase Inhibitors Leading to a Clinical Candidate for the Treatment of Acute Pancreatitis
Walker, Ann L, Ancellin, Nicolas, Beaufils, Benjamin, Bergeal, Marylise, Binnie, Margaret, Bouillot, Anne, Clapham, David, Denis, Alexis, Haslam, Carl P, Holmes, Duncan S, Hutchinson, Jonathan P, Liddle, John, McBride, Andrew, Mirguet, Olivier, Mowat, Christopher G, Rowland, Paul, Tiberghien, Nathalie, Trottet, Lionel, Uings, Iain, Webster, Scott P, Zheng, Xiaozhong, Mole, Damian J
Published in Journal of medicinal chemistry (27.04.2017)
Published in Journal of medicinal chemistry (27.04.2017)
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Design and synthesis of bridged piperidine and piperazine isosteres
Maertens, Gaëtan, Saavedra, Oscar M., Vece, Vito, Reyes, Miguel A. Vilchis, Hocine, Sofiane, Öney, Esat, Goument, Bertrand, Mirguet, Olivier, Le Tiran, Arnaud, Gloanec, Philippe, Hanessian, Stephen
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
Published in Bioorganic & medicinal chemistry letters (15.08.2018)
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A simple and efficient one-step synthesis of 3-substituted-4-hydroxyquinolin-2-one derivatives
Toum, Jérôme, Moquette, Alexandre, Lamotte, Yann, Mirguet, Olivier
Published in Tetrahedron letters (11.04.2012)
Published in Tetrahedron letters (11.04.2012)
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