Development of a Bivalent Ligand for a Chemokine Receptor CXCR4 by Utilizing Polyproline Helix as a Linker

摘要

Novel CXCR4 bivalent ligands which linked two FC131 analogues with rigid linkers were designed and synthesized. The binding of the bivalent ligands showed that the dimer of CXCR4 could be formed by TM4-5 assembly. This bivalent ligand approach could be useful for elucidation of GPCR functions.