Development and application of fluorescent SDF-1 derivatives

Future Med Chem. 2012 May;4(7):837-44. doi: 10.4155/fmc.12.31.


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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Calcium / immunology
  • Chemokine CXCL12 / analysis
  • Chemokine CXCL12 / chemical synthesis
  • Chemokine CXCL12 / chemistry*
  • Chemokine CXCL12 / immunology*
  • Cricetinae
  • Flow Cytometry
  • Fluorescent Dyes / analysis
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • Gene Expression
  • HEK293 Cells
  • Humans
  • Ligands
  • Microscopy, Confocal
  • Models, Molecular
  • Receptors, CXCR4 / analysis*
  • Receptors, CXCR4 / genetics
  • Receptors, CXCR4 / immunology*
  • Signal Transduction


  • CXCL12 protein, human
  • Chemokine CXCL12
  • Fluorescent Dyes
  • Ligands
  • Receptors, CXCR4
  • Calcium