Synthesis and application of fluorescein- and biotin-labeled molecular probes for the chemokine receptor CXCR4

Shinya Oishi, Ryo Masuda, Barry Evans, Satoshi Ueda, Yukiko Goto, Hiroaki Ohno, Akira Hirasawa, Gozoh Tsujimoto, Zixuan Wang, Stephen C. Peiper, Takeshi Naito, Eiichi Kodama, Masao Matsuoka, Nobutaka Fujii

Research output: Contribution to journalArticlepeer-review

35 Citations (Scopus)

Abstract

The design, synthesis, and bioevaluation of fluorescence- and biotin-labeled CXCR4 antagonists are described. The modification of D-Lys8 at an ε-amino group in the peptide antagonist Ac-TZ14011 derived from polyphemusin II had 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.

Original languageEnglish
Pages (from-to)1154-1158
Number of pages5
JournalChemBioChem
Volume9
Issue number7
DOIs
Publication statusPublished - 2008 May 5
Externally publishedYes

Keywords

  • CXCR4 antagonists
  • Cell imaging
  • Chemokine receptors
  • Fluorescent probes
  • Peptides

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Organic Chemistry

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