ArticleMolecular and cellular biochemistry2005
Agonist-induced phosphorylation and desensitization of the P2Y2 nucleotide receptor.
Article in Molecular and cellular biochemistry, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed.
- A genome-wide genetic screen reveals the P2Y2-integrin axis as a stabilizer of EGFR mutants in non-small cell lung cancer (NSCLC).Science advances · 2026Article
- P2YInternational journal of molecular sciences · 2025Review
- Purinergic regulation of pulmonary vascular tone.Purinergic signalling · 2024Review
- Physiology and pathophysiology of human airway mucus.Physiological reviews · 2022Review
- The P2YInternational journal of molecular sciences · 2022Article
- A novel definition and treatment of hyperinflammation in COVID-19 based on purinergic signalling.Purinergic signalling · 2022Review
- A Photo-clickable ATP-Mimetic Reveals Nucleotide Interactors in the Membrane Proteome.Cell chemical biology · 2020Article
- Article
- Downregulation of P2Y2 and HuD during the development of the enteric nervous system in fetal rats with anorectal malformations.Molecular medicine reports · 2019Article
- Excessive Extracellular ATP Desensitizes P2Y2 and P2X4 ATP Receptors Provoking Surfactant Impairment Ending in Ventilation-Induced Lung Injury.International journal of molecular sciences · 2018Review
- Distinct roles of ecto-nucleoside triphosphate diphosphohydrolase-2 (NTPDase2) in liver regeneration and fibrosis.Purinergic signalling · 2018Article
- Prostaglandin EFrontiers in pharmacology · 2017Article
- Caveolin-1 Regulates the P2Y2 Receptor Signaling in Human 1321N1 Astrocytoma Cells.The Journal of biological chemistry · 2016Article
- Purinergic receptors as potential therapeutic targets in Alzheimer's disease.Neuropharmacology · 2016Review
- Epithelial Anion Transport as Modulator of Chemokine Signaling.Mediators of inflammation · 2016Review
- ROS Production via P2Y1-PKC-NOX2 Is Triggered by Extracellular ATP after Electrical Stimulation of Skeletal Muscle Cells.PloS one · 2015Article
- Enhanced uridine adenosine tetraphosphate-induced contraction in renal artery from type 2 diabetic Goto-Kakizaki rats due to activated cyclooxygenase/thromboxane receptor axis.Pflugers Archiv : European journal of physiology · 2014Article
- 4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2YMedChemComm · 2013Article
- Proinflammatory cytokine secretion is suppressed by TMEM16A or CFTR channel activity in human cystic fibrosis bronchial epithelia.Molecular biology of the cell · 2012Article
- P2Y receptors in the mammalian nervous system: pharmacology, ligands and therapeutic potential.CNS & neurological disorders drug targets · 2012Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Purification of HA-tagged P2Y2 receptors from transfected human 1321N1 astrocytoma cells yielded a protein with a molecular size determined by SDS-PAGE to be in the range of 57-76 kDa, which is typical of membrane glycoproteins with heterogeneous complex glycosylation. The protein phosphatase inhibitor, okadaic acid, attenuated the recovery of receptor activity from the agonist-induced desensitized state, suggesting a role for P2Y2 receptor phosphorylation in desensitization. Isolation of HA-tagged P2Y2 nucleotide receptors from metabolically [32P]-labelled cells indicated a (3.8 +/- 0.2)-fold increase in the [32P]-content of the receptor after 15 min of treatment with 100 microM UTP, as compared to immunoprecipitated receptors from untreated control cells. Receptor sequestration studies indicated that approximately 40% of the surface receptors were internalized after a 15-min stimulation with 100 microM UTP. Point mutation of three potential GRK and PKC phosphorylation sites in the third intracellular loop and C-terminal tail of the P2Y2 receptor (namely, S243A, T344A, and S356A) extinguished agonist-induced receptor phosphorylation, caused a marked reduction in the efficacy of UTP to desensitize P2Y2 receptor signalling to intracellular calcium mobilization, and impaired agonist-induced receptor internalization. Activation of PKC isoforms with phorbol 12-myristate 13-acetate that caused heterologous receptor desensitization did not increase the level of P2Y2 receptor phosphorylation. Our results indicate a role for receptor phosphorylation by phorbol-insensitive protein kinases in agonist-induced desensitization of the P2Y2 nucleotide receptor.
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