ArticleBritish journal of pharmacology2007
Agonist potency at P2X7 receptors is modulated by structurally diverse lipids.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 37 citations in OpenAlex.
- Host-directed therapeutic targets in macrophages and their ligands against mycobacteria tuberculosis.Infection and immunity · 2025Review
- Review
- P2XBritish journal of pharmacology · 2024Article
- Agonists, Antagonists, and Modulators of P2X7 Receptors.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Abacavir Increases Purinergic P2X7 Receptor Activation by ATP: Does a Pro-inflammatory Synergism Underlie Its Cardiovascular Toxicity?Frontiers in pharmacology · 2021Article
- Structural and Functional Basis for Understanding the Biological Significance of P2X7 Receptor.International journal of molecular sciences · 2020Review
- P2X7 in Cancer: From Molecular Mechanisms to Therapeutics.Frontiers in pharmacology · 2020Review
- To Inhibit or Enhance? Is There a Benefit to Positive Allosteric Modulation of P2X Receptors?Frontiers in pharmacology · 2020Review
- ATP release drives heightened immune responses associated with hypertension.Science immunology · 2019Article
- Lipin-2 regulates NLRP3 inflammasome by affecting P2X7 receptor activation.The Journal of experimental medicine · 2017Article
- The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells.PloS one · 2015Article
- Plasma membrane cholesterol as a regulator of human and rodent P2X7 receptor activation and sensitization.The Journal of biological chemistry · 2014Article
- CD39 is a negative regulator of P2X7-mediated inflammatory cell death in mast cells.Cell communication and signaling : CCS · 2014Article
- Sphingosine regulates the NLRP3-inflammasome and IL-1β release from macrophages.European journal of immunology · 2012Article
- Activation and regulation of purinergic P2X receptor channels.Pharmacological reviews · 2011Review
- Clemastine potentiates the human P2X7 receptor by sensitizing it to lower ATP concentrations.The Journal of biological chemistry · 2011Article
- Lipopolysaccharide inhibits the channel activity of the P2X7 receptor.Mediators of inflammation · 2011Article
- Allosteric modulation of ATP-gated P2X receptor channels.Reviews in the neurosciences · 2011Review
- Mycobacterium tuberculosis synergizes with ATP to induce release of microvesicles and exosomes containing major histocompatibility complex class II molecules capable of antigen presentation.Infection and immunity · 2010Article
- Diadenosine homodinucleotide products of ADP-ribosyl cyclases behave as modulators of the purinergic receptor P2X7.The Journal of biological chemistry · 2010Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeThe P2X(7) receptor exhibits a high degree of plasticity with agonist potency increasing after prolonged receptor activation. In this study we investigated the ability of lipids to modulate agonist potency at P2X(7) receptors. EXPERIMENTAL APPROACH: A variety of lipids, including lysophosphatidylcholine, sphingosylphosphorylcholine and hexadecylphosphorylcholine were studied for their effect on P2X(7) receptor-stimulated ethidium bromide accumulation in cells expressing human recombinant P2X(7) receptors and on P2X(7) receptor-stimulated interleukin-1 beta (IL1 beta) release from THP-1 cells. The effects of the lipids were also assessed in radioligand binding studies on human P2X(7) receptors. KEY
resultsAt concentrations (3-30 microM) below the threshold to cause cell lysis, the lipids increased agonist potency and/or maximal effects at P2X(7) receptors in both ethidium accumulation and IL1 beta release studies. There was little structure activity relationship (SAR) for this effect and sub-lytic concentrations of Triton X-100 partially mimicked the effects of the lipids. The lipids caused cell lysis and increased intracellular calcium at higher concentrations (30-100 microM) which complicated interpretation of their effects in functional studies. However, the lipids (3-100 microM) also increased agonist potency 30-100 fold in radioligand binding studies. CONCLUSIONS AND IMPLICATIONS: This study demonstrates that a diverse range of lipids increase agonist potency at the P2X(7) receptor in functional and binding studies. The broad SAR, including the effect of Triton X-100, suggests this may reflect changes in membrane properties rather than a direct effect on the P2X(7) receptor. Since many of the lipids studied accumulate in disease states they may enhance P2X(7) receptor function under pathophysiological conditions.
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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.