ArticleThe Journal of biological chemistry2007
Conformation state-sensitive antibodies to G-protein-coupled receptors.
Article in The Journal of biological chemistry, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 61 papers.
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Who cites it
61 citing papers in PubMed, 104 citations in OpenAlex.
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- Opioid Addiction and Opioid Receptor Dimerization: Structural Modeling of the OPRD1 and OPRM1 Heterodimer and Its Signaling Pathways.International journal of molecular sciences · 2021Article
- Regulation of Opioid Receptors by Their Endogenous Opioid Peptides.Cellular and molecular neurobiology · 2021Article
- High-throughput screening and validation of antibodies against synaptic proteins to explore opioid signaling dynamics.Communications biology · 2021Article
- Hemopressin as a breakthrough for the cannabinoid field.Neuropharmacology · 2021Review
- Autoantibodies Blocking MAnnals of neurology · 2020Article
- Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.Journal of medicinal chemistry · 2020Article
- Peptides from Natural or Rationally Designed Sources Can Be Used in Overweight, Obesity, and Type 2 Diabetes Therapies.Molecules (Basel, Switzerland) · 2020Review
- Adhesion G protein-coupled receptors: opportunities for drug discovery.Nature reviews. Drug discovery · 2019Article
- A cell-cell interaction format for selection of high-affinity antibodies to membrane proteins.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Phage antibody library screening for the selection of novel high-affinity human single-chain variable fragment against gastrin receptor: an in silico and in vitro study.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2019Article
- Intracellular Peptides in Cell Biology and Pharmacology.Biomolecules · 2019Review
- Regulation of an Opioid Receptor Chaperone Protein, RTP4, by Morphine.Molecular pharmacology · 2019Article
- A novel peptide that improves metabolic parameters without adverse central nervous system effects.Scientific reports · 2017Article
- Generation of G protein-coupled receptor antibodies differentially sensitive to conformational states.PloS one · 2017Article
1 more citing papers are in PubMed but not listed here.
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
Abstract
A growing body of evidence indicates that G-protein-coupled receptors undergo complex conformational changes upon agonist activation. It is likely that the extracellular region, including the N terminus, undergoes activation-dependent conformational changes. We examined this by generating antibodies to regions within the N terminus of micro-opioid receptors. We find that antibodies to the midportion of the N-terminal tail exhibit enhanced recognition of activated receptors, whereas those to the distal regions do not. The enhanced recognition is abolished upon treatment with agents that block G-protein coupling or deglycosylate the receptor. This suggests that the N-terminal region of mu receptors undergoes conformational changes following receptor activation that can be selectively detected by these region-specific antibodies. We used these antibodies to characterize micro receptor type-specific ligands and find that the antibodies accurately differentiate ligands with varying efficacies. Next, we examined if these antibodies can be used to investigate the extent and duration of activation of endogenous receptors. We find that peripheral morphine administration leads to a time-dependent increase in antibody binding in the striatum and prefrontal cortex with a peak at about 30 min, indicating that these antibodies can be used to probe the spatio-temporal dynamics of native mu receptors. Finally, we show that this strategy of targeting the N-terminal region to generate receptor conformation-specific antisera can be applied to other G(alpha)(i)-coupled (delta-opioid, CB1 cannabinoid, alpha(2A)-adrenergic) as well as G(alpha)(s)-(beta(2)-adrenergic) and G(alpha)(q)-coupled (AT1 angiotensin) receptors. Taken together, these studies describe antisera as tools that allow, for the first time, studies probing differential conformation states of G-protein-coupled receptors, which could be used to identify molecules 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.