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Josef Vagner, Liping Xu, Heather L. Handl, Jatinder S. Josan, David L. Morse, Eugene A. Mash, Robert J. Gillies and Victor J. Hruby Heterobivalent Ligands Crosslink Multiple Cell-Surface Receptors: The Human Melanocortin-4 and δ-Opioid Receptors Angewandte Chemie International Edition 47

Article first published online: 18 JAN 2008 | DOI: 10.1002/anie.200702770

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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.

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