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Synthesis and Application of Fluorescein- and Biotin-Labeled Molecular Probes for the Chemokine Receptor CXCR4

โœ Scribed by Shinya Oishi; Ryo Masuda; Barry Evans; Satoshi Ueda; Yukiko Goto; Hiroaki Ohno; Akira Hirasawa; Gozoh Tsujimoto; Zixuan Wang; Stephen C. Peiper; Takeshi Naito; Eiichi Kodama; Masao Matsuoka; Nobutaka Fujii

Publisher
John Wiley and Sons
Year
2008
Tongue
English
Weight
412 KB
Volume
9
Category
Article
ISSN
1439-4227

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โœฆ Synopsis

Abstract

The design, synthesis, and bioevaluation of fluorescenceโ€ and biotinโ€labeled CXCR4 antagonists are described. The modification of Dโ€Lys8 at an ฮตโ€amino group in the peptide antagonist Acโ€TZ14011 derived from polyphemusin II had no significant influence on the potent binding of the peptide to the CXCR4 receptor. The application of the labeled peptides in flow cytometry and confocal microscopy studies demonstrated the selectivity of their binding to the CXCR4 receptor, but not to CXCR7, which was recently reported to be another receptor for stromal cellโ€derived factor 1 (SDFโ€1)/CXCL12.

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