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Heterobivalent Ligands Crosslink Multiple Cell‐Surface Receptors: The Human Melanocortin‐4 and δ‐Opioid Receptors
Author(s) -
Vagner Josef,
Xu Liping,
Handl Heather L.,
Josan Jatinder S.,
Morse David L.,
Mash Eugene A.,
Gillies Robert J.,
Hruby Victor J.
Publication year - 2008
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200702770
Subject(s) - receptor , chemistry , melanocortin , cooperativity , ligand (biochemistry) , opioid , binding affinities , opioid receptor , cooperative binding , fluorescence , stereochemistry , affinities , dendrimer , combinatorial chemistry , biophysics , biochemistry , binding site , biology , physics , quantum mechanics
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.