Development And Application Of Fluorescent SDF-1 Derivatives
Copyright policy )Development And Application Of Fluorescent SDF-1 Derivatives
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.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.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.
- Kyoto University Japan
- Tohoku University Japan
Models, Molecular, Fluorescent Dyes/analysis, Receptors, CXCR4, Gene Expression, CHO Cells, Ligands, Calcium/immunology, CXCR4/immunology, Chemokine CXCL12/chemical synthesis, Models, Cricetinae, Receptors, CXCR4/analysis, Animals, Humans, Fluorescent Dyes/chemistry, Fluorescent Dyes, Microscopy, Microscopy, Confocal, Chemokine CXCL12/chemistry, Molecular, Flow Cytometry, CXCR4/genetics, Chemokine CXCL12, HEK293 Cells, Confocal, Fluorescent Dyes/chemical synthesis, Chemokine CXCL12/analysis, Calcium, Chemokine CXCL12/immunology, Signal Transduction
Models, Molecular, Fluorescent Dyes/analysis, Receptors, CXCR4, Gene Expression, CHO Cells, Ligands, Calcium/immunology, CXCR4/immunology, Chemokine CXCL12/chemical synthesis, Models, Cricetinae, Receptors, CXCR4/analysis, Animals, Humans, Fluorescent Dyes/chemistry, Fluorescent Dyes, Microscopy, Microscopy, Confocal, Chemokine CXCL12/chemistry, Molecular, Flow Cytometry, CXCR4/genetics, Chemokine CXCL12, HEK293 Cells, Confocal, Fluorescent Dyes/chemical synthesis, Chemokine CXCL12/analysis, Calcium, Chemokine CXCL12/immunology, Signal Transduction
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