Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore

A highly potent CXCR4 antagonist 2 [cyclo (-D-Tyr1-Arg2-Arg3-Nal4-Gly5-)] has previously been identified by screening cyclic pentapeptide libraries that were designed based on pharmacophore residues of a 14-residue peptidic CXCR4 antagonist 1. In the present study, D-Tyr and Arg in peptide 2 were re...

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Veröffentlicht in:	Organic & biomolecular chemistry 2008-01, Vol.6 (23), p.4374
Hauptverfasser:	Tanaka, Tomohiro, Tsutsumi, Hiroshi, Nomura, Wataru, Tanabe, Yasuaki, Ohashi, Nami, Esaka, Ai, Ochiai, Chihiro, Sato, Jun, Itotani, Kyoko, Murakami, Tsutomu, Ohba, Kenji, Yamamoto, Naoki, Fujii, Nobutaka, Tamamura, Hirokazu
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Cattle Cell Line Drug Discovery HIV-1 - drug effects Humans Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Oligopeptides - toxicity Peptides, Cyclic - chemical synthesis Peptides, Cyclic - chemistry Peptides, Cyclic - pharmacology Peptides, Cyclic - toxicity Receptors, CXCR4 - antagonists & inhibitors Structure-Activity Relationship Tyrosine - chemistry
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