Blar i forfatter "Karlshøj, Stefanie"

Viser treff 1-2 av 2

    • Influence of chain length on the activity of tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4) 

      Baumann, Markus; Hussain, Mohammad Musarraf; Henne, Nina; Garrote, Daniel Moya; Karlshøj, Stefanie; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Journal article; Tidsskriftartikkel; Peer reviewed, 2016-11-21)
      Here we report a series of close analogues of our recently published scaffold-based tripeptidomimetic CXCR4 antagonists, containing positively charged guanidino groups in R1 and R2, and an aromatic group in R3. While contraction/elongation of the guanidine carrying side chains (R1 and R2) resulted in loss of activity, introduction of bromine in position 1 on the naphth-2-ylmethyl moiety (R3 ...

    • Probing the molecular interactions between CXC chemokine receptor 4 (CXCR4) and an arginine-based tripeptidomimetic antagonist (KRH-1636) 

      Zachariassen, Zack George; Karlshøj, Stefanie; Haug, Bengt Erik; Rosenkilde, Mette M.; Våbenø, Jon (Journal article; Tidsskriftartikkel; Peer reviewed, 2015-09-23)
      We here report an experimentally verified binding mode for the known tripeptidomimetic CXCR4 antagonist KRH-1636 (1). A limited SAR study based on the three functionalities of 1 was first conducted, followed by site-directed mutagenesis studies. The receptor mapping showed that both the potency and affinity of 1 were dependent on the transmembrane residues His113, Asp171, Asp262, and His281 and also ...