ArticlePurinergic signalling2014
Natural compounds with P2X7 receptor-modulating properties.
Article in Purinergic signalling, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 30 citations in OpenAlex.
- Effects of New P2X7R Antagonists on Retinal Inflammatory Degenerative Conditions.Inflammation · 2026Article
- P2 Receptors as Therapeutic Targets in Allergic Rhinitis: Insights From the Use of Natural Products and Preclinical Studies.Journal of immunology research · 2026Review
- Screening herbal and natural product libraries to aid discovery of novel allosteric modulators of human P2X7.Purinergic signalling · 2025Article
- Purine and purinergic receptors in health and disease.MedComm · 2023Review
- Tumour immune escape via P2X7 receptor signalling.Frontiers in immunology · 2023Review
- Article
- A novel definition and treatment of hyperinflammation in COVID-19 based on purinergic signalling.Purinergic signalling · 2022Review
- Antagonism of the ATP-gated P2X7 receptor: a potential therapeutic strategy for cancer.Purinergic signalling · 2021Review
- Functional P2XThe Journal of neuroscience : the official journal of the Society for Neuroscience · 2021Article
- A small-molecule P2RX7 activator promotes anti-tumor immune responses and sensitizes lung tumor to immunotherapy.Nature communications · 2021Article
- Membrane Transporters and Channels in Melanoma.Reviews of physiology, biochemistry and pharmacology · 2021Review
- Structural and Functional Basis for Understanding the Biological Significance of P2X7 Receptor.International journal of molecular sciences · 2020Review
- Involvement of P2 receptors in hematopoiesis and hematopoietic disorders, and as pharmacological targets.Purinergic signalling · 2020Review
- Therapeutic potential of natural compounds from Chinese medicine in acute and subacute phases of ischemic stroke.Neural regeneration research · 2020Review
- Bioactive Metabolites of Marine Origin Have Unusual Effects on Model Membrane Systems.Marine drugs · 2020Article
- Molecular Modeling Applied to the Discovery of New Lead Compounds for P2 Receptors Based on Natural Sources.Frontiers in pharmacology · 2020Review
- To Inhibit or Enhance? Is There a Benefit to Positive Allosteric Modulation of P2X Receptors?Frontiers in pharmacology · 2020Review
- Identification of small molecule inhibitors of the Chikungunya virus nsP1 RNA capping enzyme.Antiviral research · 2018Article
- Teniposide ameliorates bone cancer nociception in rats via the P2X7 receptor.Inflammopharmacology · 2018Article
- Genetically dissecting P2rx7 expression within the central nervous system using conditional humanized mice.Purinergic signalling · 2017Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The adenosine 5'-triphosphate (ATP)-gated P2X7 receptor is a membrane-bound, non-selective cation channel, expressed in a variety of cell types. The P2X7 senses high extracellular ATP concentrations and seems to be implicated in a wide range of cellular functions as well as pathophysiological processes, including immune responses and inflammation, release of gliotransmitters and cytokines, cancer cell growth or development of neurodegenerative diseases. In the present study, we identified natural compounds and analogues that can block or sensitize the ATP (1 mM)-induced Ca(2+) response using a HEK293 cell line stably expressing human P2X7 and fluorometric imaging plate reader technology. For instance, teniposide potently blocked the human P2X7 at sub-miromolar concentrations, but not human P2X4 or rat P2X2. A marked block of ATP-induced Ca(2+) entry and Yo-Pro-1 uptake was also observed in human A375 melanoma cells and mouse microglial cells, both expressing P2X7. On the other hand, agelasine (AGL) and garcinolic acid (GA) facilitated the P2X7 response to ATP in all three cell populations. GA also enhanced the YO-PRO-1 uptake, whereas AGL did not affect the ATP-stimulated intracellular accumulation of this dye. According to the pathophysiological role of P2X7 in various diseases, selective modulators may have potential for further development, e.g. as neuroprotective or antineoplastic drugs.
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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.