Increasing evidence has shown that chemokine receptors may form functional dimers with unique pharmacological
profiles. A common practice to characterize such G protein-coupled receptor dimerization processes is to apply bivalent
ligands as chemical probes which can interact with both receptors simultaneously. Currently, two chemokine receptor
dimers have been studied by applying bivalent compounds: the CXCR4-CXCR4 homodimer and the CCR5-MOR heterodimer.
These bivalent compounds have revealed how dimerization influences receptor function and may lead to novel
therapeutics. Future design of bivalent ligands for chemokine receptor dimers may be aided with the recently available
CXCR4 homodimer, and CCR5 monomer crystal structures by more accurately simulating chemokine receptors and their
Keywords: Bivalent ligand, CCR5, chemokine receptor, CXCR4, dimerization, GPCR, MOR.
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