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Synthesis and Application of Fluorescein‐ and Biotin‐Labeled Molecular Probes for the Chemokine Receptor CXCR4
Author(s) -
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
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700761
Subject(s) - biotin , cxcr4 , peptide , chemokine receptor , fluorescein , receptor , cxcr4 antagonist , chemistry , flow cytometry , confocal microscopy , stromal cell , biochemistry , chemokine , microbiology and biotechnology , fluorescence , biology , cancer research , physics , quantum mechanics
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.