• 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. ...
    • Zinc-Chelating Compounds as Inhibitors of Human and Bacterial Zinc Metalloproteases 

      Rahman, Fatema; Wushur, Imin; Malla, Nabin; Åstrand, Ove Alexander Høgmoen; Rongved, Pål; Winberg, Jan-Olof; Sylte, Ingebrigt (Journal article; Tidsskriftartikkel; Peer reviewed, 2021-12-22)
      Inhibition of bacterial virulence is believed to be a new treatment option for bacterial infections. In the present study, we tested dipicolylamine (DPA), tripicolylamine (TPA), tris pyridine ethylene diamine (TPED), pyridine and thiophene derivatives as putative inhibitors of the bacterial virulence factors thermolysin (TLN), pseudolysin (PLN) and aureolysin (ALN) and the human zinc metalloproteases, ...
    • ZN148 Is a Modular Synthetic Metallo-beta-Lactamase Inhibitor That Reverses Carbapenem Resistance in Gram-Negative Pathogens In Vivo 

      Samuelsen, Ørjan; Åstrand, Ove Alexander Høgmoen; Frøhlich, Christopher; Heikal, Adam; Skagseth, Susann; Carlsen, Trine Josefine Olsen; Leiros, Hanna-Kirsti S.; Bayer, Annette; Schnaars, Christian; Kildahl-andersen, Geir; Lauksund, Silje; Finke, Sarah; Huber, Sandra; Gjøen, Tor; Andresen, Adriana Magalhaes Santos; Økstad, Ole Andreas; Rongved, Pål (Journal article; Tidsskriftartikkel; Peer reviewed, 2020-05-21)
      Carbapenem-resistant Gram-negative pathogens are a critical public health threat and there is an urgent need for new treatments. Carbapenemases (β-lactamases able to inactivate carbapenems) have been identified in both serine β-lactamase (SBL) and metallo-β-lactamase (MBL) families. The recent introduction of SBL carbapenemase inhibitors has provided alternative therapeutic options. Unfortunately, ...