Blar i forfatter Det helsevitenskapelige fakultet "Thoresen, G. Hege"

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    • Synthesis, biological evaluation and molecular modeling studies of the PPARβ/δ antagonist CC618 

      Kaupang, Åsmund; Paulsen, Steinar Martin; Steindal, Calin Constantin; Ravna, Aina Westrheim; Sylte, Ingebrigt; Halvorsen, Trine Grønhaug; Thoresen, G. Hege; Hansen, Trond Vidar (Journal article; Tidsskriftartikkel; Peer reviewed, 2015-03-05)
      Abstract: Herein, we describe the synthesis, biological evaluation and molecular docking of the selective PPARb/ d antagonist (4-methyl-2-(4-(trifluoromethyl)phenyl)-N-(2-(5-(trifluoromethyl)-pyridin-2-ylsulfonyl) ethyl)thiazole-5-carboxamide)), CC618. Results from in vitro luciferase reporter gene assays against the three known human PPAR subtypes revealed that CC618 selectively antagonizes ...

    • Synthesis, in vitro and in vivo biological evaluation of new oxysterols as modulators of the liver X receptors 

      Åstrand, Ove Alexander Høgmoen; Viktorsson, Elvar Örn; Kristensen, Aleksander Lim; Ekeberg, Dag; Røberg-Larsen, Hanne; Wilson, Steven Ray Haakon; Gabrielsen, Mari; Sylte, Ingebrigt; Rustan, Arild; Thoresen, G. Hege; Rongved, Pål; Kase, Eili Tranheim (Journal article; Tidsskriftartikkel; Peer reviewed, 2016-07-26)
      Liver X Receptor (LXR) modulators have shown potential as drugs since they target genes affecting metabolism and fatty acid synthesis. LXR antagonists are of particular interest since they are able to reduce the synthesis of complex fatty acids and glucose uptake. Based on molecular modeling, five new cholesterol mimics were synthesized, where four contained a hydroxyl group in the 22-S-position. ...