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Journal of Biological Chemistry
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Phosphorylation of the δ-Opioid Receptor Regulates Its β-Arrestins Selectivity and Subsequent Receptor Internalization and Adenylyl Cyclase Desensitization

Authors: Yu Qiu; Ping-Yee Law; Horace H. Loh;

Phosphorylation of the δ-Opioid Receptor Regulates Its β-Arrestins Selectivity and Subsequent Receptor Internalization and Adenylyl Cyclase Desensitization

Abstract

In the current study, we investigated the role of receptor phosphorylation and beta-arrestins in delta-opioid receptor (DOR) signaling and trafficking by using a DOR mutant in which all Ser/Thr residues in the C terminus were mutated to Ala (DTS). We demonstrated that the DOR agonist D-[Pen(2),Pen(5)]enkephalin could induce receptor internalization and adenylyl cyclase (AC) desensitization of DTS, but with comparatively slower kinetics than those observed with wild type DOR. Blockade of the internalization of DTS by the dominant-negative mutant dynamin, dynamin K44E, did not affect AC desensitization. However, depletion of beta-arrestins almost totally blocked both internalization and AC desensitization of DTS. A BRET assay suggested that DOR phosphorylation promotes receptor selectivity for beta-arrestin 2 over beta-arrestin 1. Furthermore, in mouse embryonic fibroblast (MEF) cells lacking either beta-arrestin 1 (beta arr1(-/-)) or beta-arrestin 2 (beta arr2(-/-)), agonist-induced DTS desensitization and internalization were similar to that observed in wild type MEFs. In contrast, although DOR internalization decreased in both beta arr1(-/-) MEFs and beta arr2(-/-) MEFs, DPDPE-induced DOR desensitization was significantly reduced in beta arr2(-/-) MEFs, but not in beta arr1(-/-) MEFs. Additionally, the BRET assay suggested that depletion of phosphorylation did not influence the stability of the receptor-beta-arrestin complex. Consistent with this observation, DTS did not recycle after internalization, which is like wild type DOR. Taken together, these results indicate that receptor phosphorylation confers DOR selectivity for beta-arrestin 2 without affecting the stability of the receptor-beta-arrestin complex and the fate of the internalized receptor.

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Keywords

Dynamins, Arrestins, beta-Arrestin 2, Cell Line, Protein Structure, Tertiary, Kinetics, Mice, beta-Arrestin 1, Receptors, Opioid, delta, Receptors, Opioid, Cyclic AMP, Animals, Humans, Phosphorylation, beta-Arrestins, Adenylyl Cyclases, Genes, Dominant, Protein Binding

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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
47
Average
Top 10%
Top 10%
gold