Evidence map›Paper›PMID 18256033›Full record

ArticleThe Journal of biological chemistry2008

Post-activation-mediated changes in opioid receptors detected by N-terminal antibodies.

Achla Gupta, Raphael Rozenfeld, Ivone Gomes, Kirsten M Raehal, Fabien M Décaillot, Laura M Bohn, Lakshmi A Devi

Open access · hybridAbstract read
In one paragraph

Article in The Journal of biological chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.4field-weighted citation impact, top 20% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 24 citations in OpenAlex.

  1. Endothelin-converting enzyme 2 regulates κ opioid receptor trafficking and function.The Journal of pharmacology and experimental therapeutics · 2025
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  12. Coexpression of delta- and mu-opioid receptors in nociceptive sensory neurons.Proceedings of the National Academy of Sciences of the United States of America · 2010
    Article
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  14. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 2 institutions in 1 country.

Achla GuptaDepartment of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, New York 10029, USA.
Raphael Rozenfeld
Ivone Gomes
Kirsten M Raehal
Fabien M Décaillot
Laura M Bohn
Lakshmi A Devi
Icahn School of Medicine at Mount Sinai · USThe Ohio State University · US

Funding

Regulation Of Opioid Receptor Signaling by Endogenous PeptidesR01DA008863 · NIDA · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI Lakshmi A Devi, Elyssa Margolis · 1995 to 2026
$6.1M
Post-translational Regulation of Opioid and Cannabinoid Receptors.R37DA008863 · NIDA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI DEVI, LAKSHMI A · 2012 to 2021
$4.6M
Physiological Implications of Opioid Receptor RegulationR01DA018860 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI BOHN, LAURA M. · 2004 to 2008
$1.4M
POST-TRANSLATIONAL REGULATION OF OPIOID RECEPTORSK05DA019521 · NIDA · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI DEVI, LAKSHMI A · 2005 to 2014
$1.2M
Morphine Tolerance in Barrestin-2 KO Mice: Beyond PainK01DA014600 · NIDA · OHIO STATE UNIVERSITY · PI BOHN, LAURA M · 2002 to 2006
$674k
Post-translational regulation of opioid receptorsR56DA008863 · NIDA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI DEVI, LAKSHMI A · 2007 to 2007
$381k
Opioid-Induced Somatic Effects in Betaarrestin2-KO MiceF31DA021952 · NIDA · OHIO STATE UNIVERSITY · PI RAEHAL, KIRSTEN M · 2006 to 2007
$67k
NIDA NIH HHS DA021952NIDA NIH HHS DA08863NIDA NIH HHS DA14600NIDA NIH HHS DA18860NIDA NIH HHS DA19521NIDA NIH HHS K01 DA014600NIDA NIH HHS R01 DA018860NINDS NIH HHS NS053751
6 · The paper itself

Abstract

The majority of studies examining activity-induced conformational changes in G protein-coupled receptors have focused on transmembrane helices or intracellular regions. Relatively few studies have examined the involvement of the extracellular region in general and the N-terminal region in particular in this process. To begin to address this, we generated a series of antibodies to the N-terminal region of opioid receptors. Characterization of these antibodies revealed that they differentially recognize activated receptors. Recently, we generated monoclonal antibodies that recognize regions proximal to glycosylation sites in the receptor N terminus. Characterization of these antibodies revealed that agonist treatment leads to a decrease in epitope recognition by the antibody presumably because of a movement of the region of the N terminus proximal to glycosylation sites. The time course of the decrease in antibody recognition suggested that it could be due to a post-activation-mediated event. Examination of the involvement of receptor residues in the C-tail and beta-arrestin binding using site-directed mutagenesis and cells or tissues lacking beta-arrestin 2 suggests a role for these desensitization-related mechanisms in governing antibody binding to the receptor. Thus, these N-terminally directed antibodies can differentially recognize post-activation-mediated changes in the C-terminal (intracellular) region of the receptor. Therefore, these conformation-sensitive antibodies represent powerful reagents to probe receptor activation states and provide a potential tool for identifying and characterizing new compounds of therapeutic interest.

Indexed as

AnimalsAntibodiesAntibodies, MonoclonalArrestinsbeta-ArrestinsCHO CellsCricetinaeCricetulusDose-Response Relationship, DrugGlycosylationLigandsPhosphorylationProtein BindingProtein ConformationProtein Structure, TertiaryReceptors, OpioidAntibodiesAntibodies, MonoclonalArrestinsbeta-ArrestinsLigandsReceptors, Opioid

Identifiers

PMID18256033
PMCPMC2447646
OpenAlexW2020934028

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.