Blar i forfatter Artikler, rapporter og annet (farmasi) "Haug, Bengt Erik"

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    • Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4) 

      Zachariassen, Zack George; Thiele, Stefanie; Berg, Erik; Rasmussen, Pernille; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Journal article; Tidsskriftartikkel; Peer reviewed, 2014-07-14)

    • 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 ...

    • Progress toward rationally designed small-molecule peptide and peptidomimetic CXCR4 antagonists 

      Våbenø, Jon; Haug, Bengt Erik; Rosenkilde, Mette M. (Journal article; Tidsskriftartikkel; Peer reviewed, 2015-06)
      Over the last five years, X-ray structures of CXC chemokine receptor 4 (CXCR4) in complex with three different ligands (the small-molecule antagonist IT1t, the polypeptide antagonist CVX15, and the viral chemokine antagonist vMIP-II) have been released. In addition to the inherent scientific value of these specific X-ray structures, they (i) provide a reliable structural ...

    • Synthesis of a novel tripeptidomimetic scaffold and biological evaluation for CXC chemokine receptor 4 (CXCR4) antagonism 

      Baumann, Markus; Nome, Lina Marie; Zachariassen, Zack Georg; Karlshøj, Stepfanie; Fossen, Torgils; Rosenkilde, Mette M.; Våbenø, Jon; Haug, Bengt Erik (Journal article; Tidsskriftartikkel; Peer reviewed, 2017-05-17)
      We here report the preparation of a new 2,6,8-trisubstituted bicyclic tripeptidomimetic scaffold through TFA-mediated cyclization of a linear precursor containing three side chains. The introduction of a triphenylmethyl-protected thiol into carboxylic acid containing building blocks through sulfa Michael additions onto α,β-unsaturated hexafluoroisopropyl esters is described. The stereoselectivity ...