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Article

Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation.

Molecular pharmacology - 1 Apr 2008

Li Jian-Guo, Haines Dale S, Liu-Chen Lee-Yuan

Abstract excerpt

Ubiquitination of the human kappa opioid receptor (hKOR) expressed in Chinese hamster ovary (CHO) cells was observed in the presence of the proteasomal inhibitor N-benzoyloxycarbonyl (Z)-Leu-Leu-leucinal (MG132) and enhanced by the agonists (-)(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidiny) cyclohexyl] benzeneacetamide (U50,488H) and dynorphin A (Dyn A). The dominant-negative (DN) mutants GRK2-K220R and...

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Identifiers

PMID: 18212250
DOI: 10.1124/mol.107.042846
PMCID: PMC3489932

Genes

CYLD
GRK2

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation.PMID 18212250Read ↗

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(-)U50,488H [(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide] induces internalization and down-regulation of the human, but not the rat, kappa-opioid receptor: structural basis for the differential regulation.Semantic proximity Read ↗

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