ArticleThe Journal of biological chemistry2008
Post-activation-mediated changes in opioid receptors detected by N-terminal antibodies.
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.
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Who cites it
14 citing papers in PubMed, 24 citations in OpenAlex.
- Endothelin-converting enzyme 2 regulates κ opioid receptor trafficking and function.The Journal of pharmacology and experimental therapeutics · 2025Article
- Regulation of Opioid Receptors by Their Endogenous Opioid Peptides.Cellular and molecular neurobiology · 2021Article
- Addiction associated N40D mu-opioid receptor variant modulates synaptic function in human neurons.Molecular psychiatry · 2020Article
- In vivo epigenetic editing of Sema6a promoter reverses transcallosal dysconnectivity caused by C11orf46/Arl14ep risk gene.Nature communications · 2019Article
- Generation of G protein-coupled receptor antibodies differentially sensitive to conformational states.PloS one · 2017Article
- A6V polymorphism of the human μ-opioid receptor decreases signalling of morphine and endogenous opioids in vitro.British journal of pharmacology · 2015Article
- Endothelin-converting enzyme 2 differentially regulates opioid receptor activity.British journal of pharmacology · 2015Article
- Buprenorphine signalling is compromised at the N40D polymorphism of the human μ opioid receptor in vitro.British journal of pharmacology · 2014Article
- Opioid receptor function is regulated by post-endocytic peptide processing.The Journal of biological chemistry · 2014Article
- Interaction and regulatory functions of μ- and δ-opioid receptors in nociceptive afferent neurons.Neuroscience bulletin · 2012Review
- Human beta1-adrenergic receptor is subject to constitutive and regulated N-terminal cleavage.The Journal of biological chemistry · 2010Article
- Coexpression of delta- and mu-opioid receptors in nociceptive sensory neurons.Proceedings of the National Academy of Sciences of the United States of America · 2010Article
- Hydrogen sulphide induces micro opioid receptor-dependent analgesia in a rodent model of visceral pain.Molecular pain · 2010Article
- Role of antibodies in developing drugs that target G-protein-coupled receptor dimers.The Mount Sinai journal of medicine, New YorkReview
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
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.
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Registered trials
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.