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

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)837-844
Number of pages8
JournalFuture Medicinal Chemistry
Volume4
Issue number7
DOIs
Publication statusPublished - 2012 May
Externally publishedYes

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Tumor Cell Line
Cell Movement
Flow Cytometry
Ligands
tetramethylrhodamine

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology
  • Molecular Medicine

Cite this

Masuda, R., Oishi, S., Tanahara, N., Ohno, H., Hirasawa, A., Tsujimoto, G., ... Fujii, N. (2012). Development and application of fluorescent SDF-1 derivatives. Future Medicinal Chemistry, 4(7), 837-844. https://doi.org/10.4155/fmc.12.31

Development and application of fluorescent SDF-1 derivatives. / Masuda, Ryo; Oishi, Shinya; Tanahara, Noriko; Ohno, Hiroaki; Hirasawa, Akira; Tsujimoto, Gozoh; Kodama, Eiichi; Matsuoka, Masao; Fujii, Nobutaka.

In: Future Medicinal Chemistry, Vol. 4, No. 7, 05.2012, p. 837-844.

Research output: Contribution to journalArticle

Masuda, R, Oishi, S, Tanahara, N, Ohno, H, Hirasawa, A, Tsujimoto, G, Kodama, E, Matsuoka, M & Fujii, N 2012, 'Development and application of fluorescent SDF-1 derivatives', Future Medicinal Chemistry, vol. 4, no. 7, pp. 837-844. https://doi.org/10.4155/fmc.12.31
Masuda R, Oishi S, Tanahara N, Ohno H, Hirasawa A, Tsujimoto G et al. Development and application of fluorescent SDF-1 derivatives. Future Medicinal Chemistry. 2012 May;4(7):837-844. https://doi.org/10.4155/fmc.12.31
Masuda, Ryo ; Oishi, Shinya ; Tanahara, Noriko ; Ohno, Hiroaki ; Hirasawa, Akira ; Tsujimoto, Gozoh ; Kodama, Eiichi ; Matsuoka, Masao ; Fujii, Nobutaka. / Development and application of fluorescent SDF-1 derivatives. In: Future Medicinal Chemistry. 2012 ; Vol. 4, No. 7. pp. 837-844.
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AU - Kodama, Eiichi

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