Development of swich on-off type probes for detection of GPCR dimers

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Assembly status of G protein-coupled receptors (GPCR) on the cellular surface is of great interest because the multimerization of GPCR could play pivotal roles in cellular functions. The bivalent ligands with polyproline linkers for CXCR4 have been shown to work as molecular ruler because of the rigid structure of polyproline helices. To expand the utility of the ligands with rigid linkers and explore the possible multimeric form of GPCR, the effect of near infrared dye labeling for the poly-L-proline linkers were addressed utilizing our bivalent-type CXCR4 ligand. The poly-L-proline linkers containing the NIR-dye at the middle or end of the linkers were prepared and their fluorescent and binding properties were analyzed to produce novel detection methods with a switch-on-off type .