Structure–Activity Relationship Study of a CXC Chemokine Receptor Type 4 Antagonist, FC131, Using a Series of Alkene Dipeptide Isosteres

A structure–activity relationship study on a highly potent CXC chemokine receptor type 4 (CXCR4) antagonist, FC131 [cyclo(-d-Tyr1-Arg2-Arg3-Nal4-Gly5-)], was carried out using a series of alkene isosteres of the d-Tyr1-l/d-Arg2 dipeptide to investigate the binding mode of FC131 and its derivatives w...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-03, Vol.55 (6), p.2746-2757
Hauptverfasser:	Kobayashi, Kazuya, Oishi, Shinya, Hayashi, Ryoko, Tomita, Kenji, Kubo, Tatsuhiko, Tanahara, Noriko, Ohno, Hiroaki, Yoshikawa, Yasushi, Furuya, Toshio, Hoshino, Masaru, Fujii, Nobutaka
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkenes - chemical synthesis Alkenes - chemistry Alkenes - pharmacology Dipeptides - chemistry HEK293 Cells Humans Magnetic Resonance Spectroscopy Models, Molecular Molecular Conformation Peptides, Cyclic - chemical synthesis Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology Peptidomimetics - chemical synthesis Peptidomimetics - chemistry Peptidomimetics - pharmacology Radioligand Assay Receptors, CXCR4 - antagonists & inhibitors Static Electricity Stereoisomerism Structure-Activity Relationship
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