title: From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
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.
authors.affiliation: Lipid Metabolism Discovery Performance Unit, GlaxoSmithKline, Les Ulis Cedex, France. olivier.x.mirguet@gsk.com
authors.forename: Olivier
authors.initials: O
authors.lastname: Mirguet
authors.forename: Yann
authors.initials: Y
authors.lastname: Lamotte
authors.forename: Frédéric
authors.initials: F
authors.lastname: Donche
authors.forename: Jérôme
authors.initials: J
authors.lastname: Toum
authors.forename: Françoise
authors.initials: F
authors.lastname: Gellibert
authors.forename: Anne
authors.initials: A
authors.lastname: Bouillot
authors.forename: Romain
authors.initials: R
authors.lastname: Gosmini
authors.forename: Van-Loc
authors.initials: VL
authors.lastname: Nguyen
authors.forename: Delphine
authors.initials: D
authors.lastname: Delannée
authors.forename: Jonathan
authors.initials: J
authors.lastname: Seal
authors.forename: Florence
authors.initials: F
authors.lastname: Blandel
authors.forename: Anne-Bénédicte
authors.initials: AB
authors.lastname: Boullay
authors.forename: Eric
authors.initials: E
authors.lastname: Boursier
authors.forename: Sandrine
authors.initials: S
authors.lastname: Martin
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Brusq
authors.forename: Gael
authors.initials: G
authors.lastname: Krysa
authors.forename: Alizon
authors.initials: A
authors.lastname: Riou
authors.forename: Rémi
authors.initials: R
authors.lastname: Tellier
authors.forename: Agnès
authors.initials: A
authors.lastname: Costaz
authors.forename: Pascal
authors.initials: P
authors.lastname: Huet
authors.forename: Yann
authors.initials: Y
authors.lastname: Dudit
authors.forename: Lionel
authors.initials: L
authors.lastname: Trottet
authors.forename: Jorge
authors.initials: J
authors.lastname: Kirilovsky
authors.forename: Edwige
authors.initials: E
authors.lastname: Nicodeme
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology; D016632:Apolipoprotein A-I / Q000378:metabolism*; D055808:Drug Discovery; D056945:Hep G2 Cells; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry* / Q000494:pharmacology*; D051548:Histone Acetyltransferases; D056488:Histone Chaperones; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008807:Mice, Inbred BALB C; D009419:Nerve Tissue Proteins; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship; D015854:Up-Regulation / Q000187:drug effects*; D000092468:Bromodomain Containing Proteins
chemical_list: D000893:Anti-Inflammatory Agents; D016632:Apolipoprotein A-I; D006576:Heterocyclic Compounds, 4 or More Rings; D051548:Histone Acetyltransferases; D056488:Histone Chaperones; D009419:Nerve Tissue Proteins; D009687:Nuclear Proteins; D011804:Quinolines; C548159:BRD1 protein, rat; D000092468:Bromodomain Containing Proteins; C568713:GSK1210151A; C037219:quinoline; C402649:BRD1 protein, human