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(®) 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
authors.forename: Ryo
authors.initials: R
authors.lastname: Masuda
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Noriko
authors.initials: N
authors.lastname: Tanahara
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Ohno
authors.forename: Akira
authors.initials: A
authors.lastname: Hirasawa
authors.forename: Gozoh
authors.initials: G
authors.lastname: Tsujimoto
authors.forename: Eiichi
authors.initials: E
authors.lastname: Kodama
authors.forename: Masao
authors.initials: M
authors.lastname: Matsuoka
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
mesh_terms: D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000276:immunology; D054377:Chemokine CXCL12 / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry* / Q000276:immunology*; D006224:Cricetinae; D005434:Flow Cytometry; D005456:Fluorescent Dyes / Q000032:analysis / Q000138:chemical synthesis / Q000737:chemistry*; D015870:Gene Expression; D057809:HEK293 Cells; D006801:Humans; D008024:Ligands; D018613:Microscopy, Confocal; D008958:Models, Molecular; D019718:Receptors, CXCR4 / Q000032:analysis* / Q000235:genetics / Q000276:immunology*; D015398:Signal Transduction
chemical_list: C515255:CXCL12 protein, human; D054377:Chemokine CXCL12; D005456:Fluorescent Dyes; D008024:Ligands; D019718:Receptors, CXCR4; D002118:Calcium