Synthesis and application of fluorescein- and biotin-labeled molecular probes for the chemokine receptor CXCR4
Synthesis and application of fluorescein- and biotin-labeled molecular probes for the chemokine receptor CXCR4
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DOI：
10.1002/cbic.200700761
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发表时间：
2008-05-05
期刊：
影响因子：
3.2
通讯作者：
Fujii, Nobutaka
中科院分区：
文献类型：
--
作者：
Oishi, Shinya;Masuda, Ryo;Fujii, Nobutaka
本文介绍了荧光标记和生物素标记的CXCR4拮抗剂的设计、合成和生物评价。多聚菌素II衍生的多肽拮抗剂Ac-TZ14071的e-氨基上的D-Lys8的修饰对多肽与CXCR4受体的有效结合没有显著影响。在流式细胞仪和共聚焦显微镜研究中的应用证明了它们与CXCR4受体结合的选择性，而不是最近报道的基质细胞衍生因子1(SDF-1)/CXCL12的另一种受体CXCR7。
The design, synthesis, and bioevaluation of fluorescence- and biotin-labeled CXCR4 antagonists are described The modification Of D-Lys8 at an e-amino group in the peptide antagonist Ac-TZ14071 derived from polyphemusin II hod 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.