Heterobivalent Ligands Crosslink Multiple Cell‐Surface Receptors: The Human Melanocortin‐4 and δ‐Opioid Receptors

Abstract

Together we bind: A series of synthetic heterobivalent ligands containing a fragment of melanocyte stimulating hormone analogue MSH(7) and the δ-opioid ligand deltorphin-II has been prepared. These ligands bind with higher affinity and with apparent cooperativity to cells expressing both hMC4R and δ-opioid receptors. Binding affinities were evaluated using a lanthanide-based in-cyto time-resolved fluorescence binding assay.