• Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target 

      Tillmanns, Julia; Häge, Sigrun; Borst, Eva Maria; Wardin, Julia; Eickhoff, Jan; Klebl, Bert; Wagner, Sabrina; Wangen, Christina; Hahn, Friedrich; Socher, Eileen; Marschall, Manfred (Journal article; Tidsskriftartikkel; Peer reviewed, 2023-04-14)
      Herpesviral nuclear egress is a regulated process of viral capsid nucleocytoplasmic release. Due to the large capsid size, a regular transport via the nuclear pores is unfeasible, so that a multistageregulated export pathway through the nuclear lamina and both leaflets of the nuclear membrane has evolved. This process involves regulatory proteins, which support the local distortion of the ...
    • A highly selective purine-based inhibitor of CSF1R potently inhibits osteoclast differentiation 

      Aarhus, Thomas Ihle; Eickhoff, Jan; Klebl, Bert; Unger, Anke; Boros, Johanna; Choidas, Axel; Zischinsky, Mia-Lisa; Wolowczyk, Camilla Izabel; Bjørkøy, Geir; Sundby, Eirik; Hoff, Bård Helge (Journal article; Tidsskriftartikkel; Peer reviewed, 2023-04-28)
      The colony-stimulating factor 1 receptor (CSF1R) plays an important role in the regulation of many inflammatory processes, and overexpression of the kinase is implicated in several disease states. Identifying selective, smallmolecule inhibitors of CSF1R may be a crucial step toward treating these disorders. Through modelling, synthesis, and a systematic structure-activity relationship study, we ...
    • Kinase chemodiversity from the Arctic: the breitfussins 

      Østnes Hansen, Kine; Andersen, Jeanette hammer; Bayer, Annette; Pandey, Sunil Kumar; Lorentzen, Marianne; Jørgensen, Kåre Bredeli; Sydnes, Magne Olav; Guttormsen, Yngve; Baumann, Matthias; Koch, Uwe; Klebl, Bert; Eickhoff, Jan; Haug, Bengt Erik; Isaksson, Johan; Hansen, Espen (Journal article; Tidsskriftartikkel; Peer reviewed, 2019-10-24)
      In this work, we demonstrate that the indole-oxazole-pyrrole framework of the breitfussin family of natural products is a promising scaffold for kinase inhibition. Six new halogenated natural products, breitfussin C–H (3 – 8) were isolated and characterized from the Arctic, marine hydrozoan Thuiaria breitfussi. The structures of two of the new natural products were also confirmed by total synthesis. ...