2. Academic Validation
  3. From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151

From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151

  • Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125.
Olivier Mirguet 1,  Yann Lamotte,  Frédéric Donche,  Jérôme Toum,  Françoise Gellibert,  Anne Bouillot,  Romain Gosmini,  Van-Loc Nguyen,  Delphine Delannée,  Jonathan Seal,  Florence Blandel,  Anne-Bénédicte Boullay,  Eric Boursier,  Sandrine Martin,  Jean-Marie Brusq,  Gael Krysa,  Alizon Riou,  Rémi Tellier,  Agnès Costaz,  Pascal Huet,  Yann Dudit,  Lionel Trottet,  Jorge Kirilovsky,  Edwige Nicodeme
Affiliations

Affiliation

  • 1 Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France. olivier.x.mirguet@gsk.com
PMID: 22386529 DOI: 10.1016/j.bmcl.2012.01.125
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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