Development and application of fluorescent SDF-1 derivatives. (May 2012)

• Record Type: Journal Article
• Authors: Masuda, Ryo; Oishi, Shinya; Tanahara, Noriko; Ohno, Hiroaki; Hirasawa, Akira; Tsujimoto, Gozoh; Kodama, Eiichi; Matsuoka, Masao; Fujii, Nobutaka
• Is Part Of: Future medicinal chemistry. Volume 4:Number 7(2012)
• Page Start: 837
• Page End: 844
• Publication Date: 2012-05
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc.12.31
• Languages: English
• ISSNs: 1756-8919

Abstract

Background: SDF-1/CXCR4 signaling plays key roles in directed cell migration under physiological and pathological conditions. To develop agonist-based CXCR4 probes for detection of CXCR4 expression on cell lines and metastatic tumors, SAR analyses of fluorescent SDF-1 derivatives were carried out.Results: Several SDF-1 derivatives with a single fluorescent label were designed and synthesized. Modification of the SDF-1 C-terminus with AlexaFluor ® 488 or tetramethylrhodamine provided potent CXCR4 probes. Using a potent probe, a novel binding inhibition assay was established for biological evaluation of potential CXCR4 ligands.Conclusion: SDF-1 derivatives with C-terminal modification exhibit equipotent binding with CXCR4 and an alternative SDF-1 receptor CXCR7 to unlabeled SDF-1. The SDF-1 derivatives are applicable to flow cytometry to detect the receptor expression and identify binding compounds for CXCR4.