ArticlePurinergic signalling2020
P2X7 receptor antagonism inhibits tumour growth in human high-grade gliomas.
Article in Purinergic signalling, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 42 citations in OpenAlex.
- Radioiodinated compound FJR01: a novel P2X7R-targeted SPECT tracer for visualizing glioma-associated microglia/macrophages in a rat glioblastoma model.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- Tumor growth inhibitory activity of the P2X7 receptor antagonist AZ10606120 in two cell lines of human glioblastoma.Purinergic signalling · 2026Article
- P2X7 receptor: a potential therapeutic target for chronic respiratory diseases.Molecular and cellular biochemistry · 2026Review
- Expression and Functional Role of the P2X7 Receptor in Glioma Models and Tissues: A Systematic Review.Cancers · 2025Review
- Targeting Gliomas with Beta-Amyloid-Specific Dyes: A Novel Approach for In Vivo Staining and Potential Therapeutic Applications.International journal of molecular sciences · 2025Article
- Characterisation of the expression of P2X7 receptor, cancer stem cell markers and immunological mediators in human high-grade gliomas.BMC neuroscience · 2025Article
- Functional role of P2X7 purinergic receptor in cancer and cancer-related pain.Purinergic signalling · 2025Review
- Purines and purinergic receptors in primary tumors of the central nervous system.Purinergic signalling · 2025Article
- Article
- Role of P2X7 receptor in the progression and clinicopathological characteristics of gastric cancer.Scientific reports · 2024Article
- P2X7R Modulates NEK7-NLRP3 Interaction to Exacerbate Experimental Autoimmune Prostatitis via GSDMD-mediated Prostate Epithelial Cell Pyroptosis.International journal of biological sciences · 2024Article
- Machine learning discriminates P2X7-mediated intracellular calcium sparks in human-induced pluripotent stem cell-derived neural stem cells.Scientific reports · 2023Article
- P2X7 receptor antagonism by AZ10606120 significantly reduced in vitro tumour growth in human glioblastoma.Scientific reports · 2023Article
- Synthesis, Biological Evaluation and Molecular Modeling Studies of Naphthoquinone Sulfonamides and Sulfonate Ester Derivatives as P2X7 Inhibitors.Molecules (Basel, Switzerland) · 2023Article
- Purinergic signaling: Diverse effects and therapeutic potential in cancer.Frontiers in oncology · 2023Review
- Interactions between microglia and glioma in tumor microenvironment.Frontiers in oncology · 2023Review
- Synthesis, biological evaluation and molecular modeling studies of novel 1,2,3-triazole-linked menadione-furan derivatives as P2X7 inhibitors.Journal of bioenergetics and biomembranes · 2022Article
- Neurotransmitters: Potential Targets in Glioblastoma.Cancers · 2022Review
- Alternatively Spliced Isoforms of the P2X7 Receptor: Structure, Function and Disease Associations.International journal of molecular sciences · 2022Review
- P2X7 receptor: the regulator of glioma tumor development and survival.Purinergic signalling · 2022Article
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Authors and funding
6 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gliomas, the most common primary brain cancer, are highly infiltrative and extremely difficult to treat. Despite advancements, current treatment is limited, with patients surviving for a median of 14-15 months post-diagnosis. Previous research has demonstrated the upregulation of a purinergic receptor, P2X7R, in human gliomas. P2X7R is expressed on both glioma cells and microglia within the glioma microenvironment. It is hypothesized that P2X7R contributes to tumour growth and proliferation via immune-mediated mechanisms involving tumour cells and surrounding microglia. We sought to elucidate the role of P2X7R in a human glioblastoma cell line (U251) and on surgically resected human glioma samples. We treated U251 and human glioma cultures for 72 h with P2X7R antagonists, Brilliant Blue G (BBG), oxidized ATP (oATP) and AZ10606120. Cell counting via fluorescence confocal microscopy was conducted to assess tumour proliferation. We observed no significant reductions in tumour cell numbers following P2X7R antagonism with BBG (20 μM) and oATP (250 μM) in both U251 cells and human glioma samples. Interestingly, there was a significant reduction in tumour cell number in both U251 cells (p = 0.0156) and human glioma samples (p = 0.0476) treated with varying concentrations of AZ10606120. When compared with the conventional chemotherapeutic agent, temozolomide, AZ10606120 was also found to more effectively inhibit tumour proliferation in U251 cells (p < 0.0001). Our pilot results demonstrate a potential trophic role of P2X7R where its inhibition by AZ10606120, a potent antagonist, hinders glioma growth directly or through the inactivation of microglia. This sheds new light on P2X7R as a therapeutic target for human gliomas.
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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 Socratic graph.