Ligands regulate cell surface level of the human kappa opioid receptor by activation-induced down-regulation and pharmacological chaperone-mediated enhancement: differential effects of nonpeptide and peptide agonists.

@article{Chen2006LigandsRC,
  title={Ligands regulate cell surface level of the human kappa opioid receptor by activation-induced down-regulation and pharmacological chaperone-mediated enhancement: differential effects of nonpeptide and peptide agonists.},
  author={Yong Chen and Chongguang Chen and Yulin Wang and Lee-Yuan Liu-Chen},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2006},
  volume={319 2},
  pages={765-75}
}
Two peptide agonists, eight nonpeptide agonists, and five nonpeptide antagonists were evaluated for their capacity to regulate FLAG (DYKDDDDK)-tagged human kappa opioid receptors (hKORs) stably expressed in Chinese hamster ovary cells after incubation for 4 h with a ligand at a concentration approximately 1000-fold of its EC(50) (agonist) or K(i) (antagonist) value. Dynorphins A and B decreased the fully glycosylated mature form (55-kDa) of FLAG-hKOR by 70%, whereas nonpeptide full agonists [2… CONTINUE READING

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