Blar i forfatter "Zachariassen, Zack George"
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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) -
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 ... -
Structure-activity relationship studies of the aromatic positions in cyclopentapeptide CXCR4 antagonists
Mungalpara, Jignesh; Zachariassen, Zack George; Thiele, Stefanie; Rosenkilde, MM; Våbenø, Jon (Journal article; Tidsskriftartikkel; Peer reviewed, 2013)The cyclopentapeptide CXCR4 antagonist FC131 (cyclo(-Arg1-Arg2-2-Nal3-Gly4-D-Tyr5-), 2; 2-Nal = 3-(2-naphthyl)alanine) represents an excellent starting point for development of novel drug-like ligands with therapeutic potential in HIV, cancer, stem-cell mobilization, inflammation, and autoimmune diseases. While the structure–activity relationships for Arg1, Arg2, and Gly4 are well established, less ... -
Toward Tripeptidomimetic CXCR4 Antagonists: Design, Synthesis, Biological Evaluation, and Binding Mode Studies
Zachariassen, Zack George (Doctoral thesis; Doktorgradsavhandling, 2014-04-11)In order for the HIV virus to take over and destroy human immune cells, which results in AIDS, the virus first has to enter the cells. This takes place by interactions between viral proteins and specific receptors on the surface of our cells. One of these receptors is CXCR4, and it has been shown that chemical compounds that bind to and block the CXCR4 receptor, so-called CXCR4 antagonists, are able ...