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Title: Development and application of fluorescent SDF-1 derivatives.
Authors: Masuda, Ryo
Oishi, Shinya  kyouindb  KAKEN_id  orcid (unconfirmed)
Tanahara, Noriko
Ohno, Hiroaki  kyouindb  KAKEN_id  orcid (unconfirmed)
Hirasawa, Akira  kyouindb  KAKEN_id  orcid (unconfirmed)
Tsujimoto, Gozoh
Kodama, Eiichi
Matsuoka, Masao  KAKEN_id
Fujii, Nobutaka  KAKEN_id
Author's alias: 大石, 真也
Issue Date: May-2012
Publisher: Future Science Ltd.
Journal title: Future medicinal chemistry
Volume: 4
Issue: 7
Start page: 837
End page: 844
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.
Rights: © 2012 Future Science Ltd.
This is not the published version. Please cite only the published version.
DOI(Published Version): 10.4155/fmc.12.31
PubMed ID: 22571609
Appears in Collections:Journal Articles

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