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

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

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...

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Veröffentlicht in:Angewandte Chemie (International ed.) 2008-01, Vol.47 (9), p.1685-1688
Hauptverfasser: Vagner, Josef, Xu, Liping, Handl, Heather L, Josan, Jatinder S, Morse, David L, Mash, Eugene A, Gillies, Robert J, Hruby, Victor J
Format: Artikel
Sprache:eng
Schlagworte:
binding assay
Binding, Competitive
Circular Dichroism
Computer Simulation
fluorescence spectroscopy
Humans
Ligands
Models, Molecular
molecular dynamics
Monte Carlo Method
peptidomimetics
Receptor, Melanocortin, Type 4 - metabolism
Receptors, Opioid, delta - metabolism
solid-phase synthesis
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Zusammenfassung: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200702770