Development and application of fluorescent SDF-1 derivatives

Ryo Masuda; Shinya Oishi; Noriko Tanahara; Hiroaki Ohno; Akira Hirasawa; Gozoh Tsujimoto; Eiichi Kodama; Masao Matsuoka; Nobutaka Fujii

doi:10.4155/fmc.12.31

Development and application of fluorescent SDF-1 derivatives

Ryo Masuda, Shinya Oishi^*, Noriko Tanahara, Hiroaki Ohno, Akira Hirasawa, Gozoh Tsujimoto, Eiichi Kodama, Masao Matsuoka, Nobutaka Fujii

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

4 Citations (Scopus)

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.

Original language	English
Pages (from-to)	837-844
Number of pages	8
Journal	Future Medicinal Chemistry
Volume	4
Issue number	7
DOIs	https://doi.org/10.4155/fmc.12.31
Publication status	Published - 2012 May
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Pharmacology
Drug Discovery

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title = "Development and application of fluorescent SDF-1 derivatives",

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 {\textregistered} 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.",

author = "Ryo Masuda and Shinya Oishi and Noriko Tanahara and Hiroaki Ohno and Akira Hirasawa and Gozoh Tsujimoto and Eiichi Kodama and Masao Matsuoka and Nobutaka Fujii",

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T1 - Development and application of fluorescent SDF-1 derivatives

AU - Masuda, Ryo

AU - Oishi, Shinya

AU - Tanahara, Noriko

AU - Ohno, Hiroaki

AU - Hirasawa, Akira

AU - Tsujimoto, Gozoh

AU - Kodama, Eiichi

AU - Matsuoka, Masao

AU - Fujii, Nobutaka

PY - 2012/5

Y1 - 2012/5

N2 - 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.

AB - 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.

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Development and application of fluorescent SDF-1 derivatives

Abstract

ASJC Scopus subject areas

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