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From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151 |
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| Authors: | 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 |
| Institution: | Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France. olivier.x.mirguet@gsk.com |
| Abstract: | The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2. |
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