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

*この研究の対応する著者

研究成果: Article査読

4 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)837-844
ページ数8
ジャーナルFuture Medicinal Chemistry
4
7
DOI
出版ステータスPublished - 2012 5
外部発表はい

ASJC Scopus subject areas

  • 分子医療
  • 薬理学
  • 創薬

フィンガープリント

「Development and application of fluorescent SDF-1 derivatives」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル