FEBS Letters · 1996 · 59 citations · 23 references
MedicineMolecular BiologyPharmacologyCell SignalingMolecular PharmacologySignal TransductionDrug-receptor InteractionsLigand BindingOpioid AnalgesicsOpioid PharmacologyReceptor PharmacologyAntagonist PotencyEndogenous OpioidsMu Opioid Receptor SignalingOpioid Peptide PharmacologyOpioid Receptor AgonistsOpioid Receptor BindingPharmacological ProfilingSaturable Binding
The human mu-opioid receptor cDNA from which the 32 amino-terminal codons were substituted by the Saccharomyces cerevisiae alpha-mating factor signal sequence has been expressed in the methylotrophic yeast Pichia pastoris using the host promoter of the alcohol oxidase-1 gene. Cell membranes exhibited specific and saturable binding of the opioid antagonist [3H]diprenorphine (Kd = 0.2 nM and Bmax = 400 fmol/mg protein or 800 sites/cell). Competition studies with non-selective, and mu-, delta- and kappa-selective opioid agonists and antagonists revealed a typical mu-opioid receptor binding profile, suggesting proper folding of the protein in yeast membranes.
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Molecular cloning and functional expression of a mu opioid receptor from rat brain
Yan Chen, Anton Mestek, Jian Liu et al. · Regulatory Peptides · 1994 · 810 citations
Pharmacological characterization of the cloned kappa-, delta-, and mu-opioid receptors.
K Raynor, Hyesik Kong, Yong Chen et al. · Molecular Pharmacology · 1994 · 663 citations · Full text