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J. Biol. Chem., Vol. 269, Issue 48, 30195-30199, Dec, 1994
JC Xue, C Chen, J Zhu, S Kunapuli, JK DeRiel, L Yu and LY Liu-Chen
This study was to identify specific regions in kappa opioid receptors that
accounted for binding selectivity of kappa ligands. Six chimeric mu/kappa
receptors were constructed from cloned rat kappa and mu opioid receptors
and transiently expressed in COS-1 cells. All six chimeric mu/kappa
receptors bound [3H] diprenorphine with high affinities, indicating that
these chimeras retain opioid receptor conformation. Binding affinities of
three peptide ligands (dynorphin A, alpha-neo- endorphin, and dynorphin B)
and three nonpeptide ligands (norbinaltorphimine, U50,488H, and U69,593)
for chimeras were determined and compared to those for mu and kappa opioid
receptors. The second extracellular loop and the adjoining C-terminal
portion of the fourth transmembrane helix were essential for the high
affinity binding of dynorphin A, alpha-neo-endorphin, and dynorphin B to
the kappa receptor. The third extracellular loop and the sixth and seventh
transmembrane helices played an important role in determining the
selectivity of nor-binaltorphimine for the kappa over the mu receptor.
U50,488H and U69,593 appeared to require the whole kappa receptor except
the second extracellular loop to attain high affinity binding. Thus, the
kappa opioid receptor has differential binding domains for peptide and
non-peptide ligands.
Differential binding domains of peptide and non-peptide ligands in the cloned rat kappa opioid receptor
Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140.
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