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

The design, synthesis, and bioevaluation of fluorescence- and biotin-labeled CXCR4 antagonists are described. The modification of D-Lys8 at an ε-amino group in the peptide antagonist Ac-TZ14011 derived from polyphemusin II had no significant influence on the potent binding of the peptide to the CXCR...

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Bibliographic Details
Published in:Chembiochem : a European journal of chemical biology 2008-05, Vol.9 (7), p.1154-1158
Main Authors: Oishi, Shinya, Masuda, Ryo, Evans, Barry, Ueda, Satoshi, Goto, Yukiko, Ohno, Hiroaki, Hirasawa, Akira, Tsujimoto, Gozoh, Wang, Zixuan, Peiper, Stephen C, Naito, Takeshi, Kodama, Eiichi, Matsuoka, Masao, Fujii, Nobutaka
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Biotin - chemistry
cell imaging
Cell Line
chemokine receptors
CXCR4 antagonists
Flow Cytometry
Fluorescein - chemistry
Fluorescence
Fluorescent Dyes - analysis
Fluorescent Dyes - chemical synthesis
Fluorescent Dyes - chemistry
fluorescent probes
Inhibitory Concentration 50
Microscopy, Confocal
peptides
Peptides - analysis
Peptides - chemical synthesis
Peptides - chemistry
Peptides - pharmacology
Receptors, CXCR4 - analysis
Receptors, CXCR4 - antagonists & inhibitors
Receptors, CXCR4 - metabolism
Substrate Specificity
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Description
Summary:The design, synthesis, and bioevaluation of fluorescence- and biotin-labeled CXCR4 antagonists are described. The modification of D-Lys8 at an ε-amino group in the peptide antagonist Ac-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 cell-derived factor 1 (SDF-1)/CXCL12.
ISSN:1439-4227
1439-7633
DOI:10.1002/cbic.200700761