ArticleBritish journal of pharmacology2003
Agonist- and antagonist-induced sequestration/internalization of neuropeptide Y Y1 receptors in HEK293 cells.
Article in British journal of pharmacology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 67 citations in OpenAlex.
- Selective Receptor Modulation by Truncated Neuropeptide Y (3-36) Dissociates Vasoconstriction from Neuroprotection in Experimental Glaucoma.Molecular neurobiology · 2025Article
- Design, Synthesis, and Biological Evaluation of the First Radio-Metalated Neurotensin Analogue Targeting Neurotensin Receptor 2.ACS omega · 2023Article
- Distinct In Vitro Binding Profile of the Somatostatin Receptor Subtype 2 Antagonist [Pharmaceuticals (Basel, Switzerland) · 2021Article
- Determination of neuropeptide Y Y1 receptor antagonist BIBP 3226 and evaluation of receptor expression based on liquid chromatography coupled with tandem mass spectrometry.Analytical and bioanalytical chemistry · 2020Article
- Effects of monoclonal antagonist antibodies on calcitonin gene-related peptide receptor function and trafficking.The journal of headache and pain · 2019Article
- Visualization of ligand-induced dopamine DScientific reports · 2017Article
- Tumor Targeting and Pharmacokinetics of a Near-Infrared Fluorescent-Labeled δ-Opioid Receptor Antagonist Agent, Dmt-Tic-Cy5.Molecular pharmaceutics · 2016Article
- Neuropeptide Y receptors: a promising target for cancer imaging and therapy.Regenerative biomaterials · 2015Article
- The atypical antipsychotics clozapine and olanzapine promote down-regulation and display functional selectivity at human 5-HT7 receptors.British journal of pharmacology · 2015Article
- Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- Internalization of the human nicotinic acid receptor GPR109A is regulated by G(i), GRK2, and arrestin3.The Journal of biological chemistry · 2010Article
- Quantitative analysis of neuropeptide Y receptor association with beta-arrestin2 measured by bimolecular fluorescence complementation.British journal of pharmacology · 2010Article
- Illuminating the life of GPCRs.Cell communication and signaling : CCS · 2009Article
- Functional characterization of human variants of the mu-opioid receptor gene.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Neuropeptide Y overexpression using recombinant adeno-associated viral vectors.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2009Review
- Topical application of entry inhibitors as "virustats" to prevent sexual transmission of HIV infection.Retrovirology · 2008Review
- The Anti-Cancer Effect of AImmunology, endocrine & metabolic agents in medicinal chemistry · 2007Article
- Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors.Proceedings of the National Academy of Sciences of the United States of America · 2006Article
- BODIPY-conjugated neuropeptide Y ligands: new fluorescent tools to tag Y1, Y2, Y4 and Y5 receptor subtypes.British journal of pharmacology · 2005Article
- Juxtacellular recording/labeling analysis of physiological and anatomical characteristics of rat intergeniculate leaflet neurons.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2005Article
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1 Neuropeptide Y Y(1) receptors are known to internalize following the binding of agonists. In the present study, a pseudopeptide Y(1) receptor antagonist, homodimeric Ile-Glu-Pro-Dpr-Tyr-Arg-Leu-Arg-Tyr-CONH(2) (GR231118), also induced Y(1) receptor internalization in human embryonic kidney (HEK293) cells. 2 We demonstrated first that both specifically bound radiolabeled antagonist ([(125)I]GR231118) and agonist ([(125)I][Leu(31), Pro(34)]PYY) underwent receptor-mediated sequestration/internalization in transfected HEK293 cells. 3 Agonist-induced Y(1) receptor internalization was dependent on clathrin-coated pits and was regulated in part by Gi/o-protein activation as revealed by pertussin toxin sensitivity. In contrast, antagonist-induced sequestration of Y(1) receptors was partly dependent on clathrin-coated pits, but independent from Gi/o-protein activation. 4 Exposure to high concentrations of agonist or antagonist caused a 50 and 75% loss of cell surface binding, respectively. The loss caused by the agonist rapidly recovered. This phenomenon was blocked by monensin, an inhibitor of endosome acidification, suggesting that cell surface receptor recovery is due to recycling. In contrast to the agonist, GR231118 induced a long-lasting sequestration of Y(1) receptors in HEK293 cells. 5 Immunofluorescence labeling indicated that following 40 min of incubation with either the agonist or the antagonist, Y(1) receptors followed markedly different intercellular trafficking pathways. 6 Taken together, these findings provided evidence that a pseudopeptide Y(1) receptor antagonist can induce long-lasting disappearance of cell surface receptors through a pathway distinct from the classical endocytic/recycling pathway followed by stimulation with an agonist.
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