Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist

Edita Navratilova; Eva V. Varga; Dagmar Stropova; Janelle C. Jambrosic; William R. Roeske; Henry I. Yamamura

doi:10.1016/j.ejphar.2003.11.067

Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist

Edita Navratilova, Eva V. Varga, Dagmar Stropova, Janelle C. Jambrosic, William R. Roeske, Henry I. Yamamura

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Abstract

Chemically distinct opioid agonists have different abilities to down-regulate opioid receptors. The present study investigated the role of Ser³⁶³ in human δ-opioid receptor down-regulation by a δ-selective peptide- and non-peptide agonist. Cyclic[D-Pen ²,D-Pen⁵]enkephalin (DPDPE)-mediated down-regulation was significantly attenuated by a S363A mutation. In contrast, this mutation had no effect on down-regulation by (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5- dimethyl-1-piperazinyl)-3-methoxybenzyl]N,N-diethylbenzamide (SNC80). These results demonstrate that the molecular mechanism of the human δ-opioid receptor down-regulation is agonist-specific.

Original language	English (US)
Pages (from-to)	341-343
Number of pages	3
Journal	European Journal of Pharmacology
Volume	485
Issue number	1-3
DOIs	https://doi.org/10.1016/j.ejphar.2003.11.067
State	Published - Feb 6 2004

Keywords

Down-regulation
Trafficking, agonist-directed
δ-Opioid receptor

ASJC Scopus subject areas

Pharmacology

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10.1016/j.ejphar.2003.11.067

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@article{183be0ce87d842cca9ed27cabe52008a,

title = "Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist",

abstract = "Chemically distinct opioid agonists have different abilities to down-regulate opioid receptors. The present study investigated the role of Ser363 in human δ-opioid receptor down-regulation by a δ-selective peptide- and non-peptide agonist. Cyclic[D-Pen 2,D-Pen5]enkephalin (DPDPE)-mediated down-regulation was significantly attenuated by a S363A mutation. In contrast, this mutation had no effect on down-regulation by (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5- dimethyl-1-piperazinyl)-3-methoxybenzyl]N,N-diethylbenzamide (SNC80). These results demonstrate that the molecular mechanism of the human δ-opioid receptor down-regulation is agonist-specific.",

keywords = "Down-regulation, Trafficking, agonist-directed, δ-Opioid receptor",

author = "Edita Navratilova and Varga, {Eva V.} and Dagmar Stropova and Jambrosic, {Janelle C.} and Roeske, {William R.} and Yamamura, {Henry I.}",

note = "Funding Information: The authors thank Michelle Thatcher and Carol Haussler for maintaining the cell cultures. This work was supported by a grant from the National Institute of Health.",

year = "2004",

month = feb,

day = "6",

doi = "10.1016/j.ejphar.2003.11.067",

language = "English (US)",

volume = "485",

pages = "341--343",

journal = "European Journal of Pharmacology",

issn = "0014-2999",

publisher = "Elsevier B.V.",

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TY - JOUR

T1 - Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist

AU - Navratilova, Edita

AU - Varga, Eva V.

AU - Stropova, Dagmar

AU - Jambrosic, Janelle C.

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: The authors thank Michelle Thatcher and Carol Haussler for maintaining the cell cultures. This work was supported by a grant from the National Institute of Health.

PY - 2004/2/6

Y1 - 2004/2/6

N2 - Chemically distinct opioid agonists have different abilities to down-regulate opioid receptors. The present study investigated the role of Ser363 in human δ-opioid receptor down-regulation by a δ-selective peptide- and non-peptide agonist. Cyclic[D-Pen 2,D-Pen5]enkephalin (DPDPE)-mediated down-regulation was significantly attenuated by a S363A mutation. In contrast, this mutation had no effect on down-regulation by (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5- dimethyl-1-piperazinyl)-3-methoxybenzyl]N,N-diethylbenzamide (SNC80). These results demonstrate that the molecular mechanism of the human δ-opioid receptor down-regulation is agonist-specific.

AB - Chemically distinct opioid agonists have different abilities to down-regulate opioid receptors. The present study investigated the role of Ser363 in human δ-opioid receptor down-regulation by a δ-selective peptide- and non-peptide agonist. Cyclic[D-Pen 2,D-Pen5]enkephalin (DPDPE)-mediated down-regulation was significantly attenuated by a S363A mutation. In contrast, this mutation had no effect on down-regulation by (+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5- dimethyl-1-piperazinyl)-3-methoxybenzyl]N,N-diethylbenzamide (SNC80). These results demonstrate that the molecular mechanism of the human δ-opioid receptor down-regulation is agonist-specific.

KW - Down-regulation

KW - Trafficking, agonist-directed

KW - δ-Opioid receptor

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AN - SCOPUS:1642538355

SN - 0014-2999

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SP - 341

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JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1-3

ER -

Mutation S363A in the human δ-opioid receptor selectively reduces down-regulation by a peptide agonist

Abstract

Keywords

ASJC Scopus subject areas

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