ArticleThe Journal of biological chemistry2005
Disruption of lipid rafts inhibits P2X1 receptor-mediated currents and arterial vasoconstriction.
Article in The Journal of biological chemistry, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 102 citations in OpenAlex.
- Heat shock protein 90 inhibitors reduce trafficking of ATP-gated P2X1 receptors and human platelet responsiveness.The Journal of biological chemistry · 2012Trial
- Structural basis for a central permeation pathway in the P2X1 receptor.Cell discovery · 2026Article
- Structural basis of the multiple ligand binding mechanisms of the P2X1 receptor.Acta pharmacologica Sinica · 2025Article
- Cryo-EM structures of the human P2X1 receptor reveal subtype-specific architecture and antagonism by supramolecular ligand-binding.Nature communications · 2024Article
- Contractility defects hinder glycoprotein VI-mediated platelet activation and affect platelet functions beyond clot contraction.Research and practice in thrombosis and haemostasis · 2024Article
- Cholesterol- and actin-centered view of the plasma membrane: updating the Singer-Nicolson fluid mosaic model to commemorate its 50th anniversaryMolecular biology of the cell · 2023Article
- Regulation of P2X1 receptors by modulators of the cAMP effectors PKA and EPAC.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Purinergic signalling in the cardiovascular system-a tribute to Geoffrey Burnstock.Purinergic signalling · 2021Article
- Isolation of Lipid Rafts by the Detergent-Based and Non-detergent-Based Methods for Localization of GPCRs with Immunoblotting and Laser Scanning Confocal Microscopy.Methods in molecular biology (Clifton, N.J.) · 2021Article
- Purinergic Signaling in Controlling Macrophage and T Cell Functions During Atherosclerosis Development.Frontiers in immunology · 2020Review
- Purinergic Signaling During Hyperglycemia in Vascular Smooth Muscle Cells.Frontiers in endocrinology · 2020Review
- Development of a P2X1-eYFP receptor knock-in mouse to track receptors in real time.Purinergic signalling · 2019Article
- Phosphatidylinositol 4,5-bisphosphate, cholesterol, and fatty acids modulate the calcium-activated chloride channel TMEM16A (ANO1).Biochimica et biophysica acta. Molecular and cell biology of lipids · 2018Article
- Hyperthermia and associated changes in membrane fluidity potentiate P2X7 activation to promote tumor cell death.Oncotarget · 2017Article
- Pentosan polysulfate preserves renal microvascular P2X1 receptor reactivity and autoregulatory behavior in DOCA-salt hypertensive rats.American journal of physiology. Renal physiology · 2016Article
- Insulin-response epigenetic activation of Egr-1 and JunB genes at the nuclear periphery by A-type lamin-associated pY19-Caveolin-2 in the inner nuclear membrane.Nucleic acids research · 2015Article
- Plasma membrane cholesterol as a regulator of human and rodent P2X7 receptor activation and sensitization.The Journal of biological chemistry · 2014Article
- The purinergic neurotransmitter revisited: a single substance or multiple players?Pharmacology & therapeutics · 2014Review
- Post-translational regulation of P2X receptor channels: modulation by phospholipids.Frontiers in cellular neuroscience · 2013Review
- The trafficking and targeting of P2X receptors.Frontiers in cellular neuroscience · 2013Review
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
P2X1 receptors for ATP are ligand-gated cation channels expressed on a range of smooth muscle preparations and blood platelets. The receptors appear to be clustered close to sympathetic nerve varicosities and mediate the underlying membrane potential changes and constriction following nerve stimulation in a range of arteries and resistance arterioles. In this study we have used discontinuous sucrose density gradients, Western blot analysis, and cholesterol measurements to show that recombinant and smooth muscle (rat tail artery, vas deferens, and bladder) P2X1 receptors are present in cholesterol-rich lipid rafts and co-localize with the lipid raft markers flotillin-1 and -2. Lipid rafts are specialized lipid membrane microdomains involved in signaling and trafficking. To determine whether lipid raft association was essential for P2X1 receptor channel function we used the cholesterol-depleting agent methyl-beta-cyclodextrin (10 mm for 1 h). This led to a redistribution of the P2X1 receptor throughout the sucrose gradient and reduced P2X1 receptor-mediated (alpha,beta-methylene ATP, 10 microm) currents in HEK293 cells by >90% and contractions of the rat tail artery by approximately 50%. However contractions evoked by potassium chloride (60 mm) were unaffected by methyl-beta-cyclodextrin and the inactive analogue alpha-cyclodextrin had no effect on P2X1 receptor-mediated currents or contractions. P2X1 receptors are subject to ongoing regulation by receptors and kinases, and the present results suggest that lipid rafts are an essential component in the maintenance of these localized signaling domains and play an important role in P2X1 receptor-mediated control of arteries.
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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.