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Probing the molecular interactions between CXC chemokine receptor 4 (CXCR4) and an arginine-based tripeptidomimetic antagonist (KRH-1636)
(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 ...
Design, synthesis, and biological evaluation of scaffold-based tripeptidomimetic antagonists for CXC chemokine receptor 4 (CXCR4)
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-07-14)
Structure-activity relationship studies of the aromatic positions in cyclopentapeptide CXCR4 antagonists
(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 ...