• 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 ...
    • Two Isomeric C16 Oxo-Fatty Acids from the Diatom Chaetoceros karianus Show Dual Agonist Activity towards Human Peroxisome Proliferator-Activated Receptors (PPARs) α/γ 

      Moldes-Anaya, Angel; Sæther, Thomas; Uhlig, Silvio; Nebb, Hilde Irene; Larsen, Terje; Eilertsen, Hans Christian; Paulsen, Steinar Martin (Journal article; Tidsskriftartikkel; Peer reviewed, 2017-05-25)
      The peroxisome proliferator-activated receptors (PPARs) function as ligand-activated transcription factors that convert signals in the form of lipids to physiological responses through the activation of metabolic target genes. Due to their key roles in lipid and carbohydrate metabolism, the PPARs are important drug targets. However, for several of the PPAR drugs currently in use, adverse side effects ...