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The Elusive P2X7 Macropore
Francesco Di Virgilio1, Günther Schmalzing2, Fritz Markwardt3
1Department of Morphology, Surgery and Experimental Medicine, University of Ferrara, Ferrara, Italy.
Abstract:
ATP, which is released under pathological conditions and is considered a damage-associated molecular pattern (DAMP), activates P2X7 receptors (P2X7Rs), trimeric plasma membrane ion channels selective for small cations. P2X7Rs are partners in NOD-like receptor containing a pyrin (NLRP3) inflammasome activation and promoters of tumor cell growth. P2X7R overstimulation triggers the ATP-dependent opening of a nonselective plasma membrane pore, known as a 'macropore', which allows fluxes of large hydrophilic molecules. The pathophysiological functions of P2X7R are thought to be dependent on activation of this conductance pathway, yet its molecular identity is unknown. Recent reports show that P2X7R permeability to organic solutes is an early and intrinsic property of the channel itself. A better understanding of P2X7R-dependent changes in plasma membrane permeability will allow a rationale development of novel anti-inflammatory and anticancer drugs.
Insights
Extracellular ATP activates P2X7 receptors (P2X7Rs), leading to plasma membrane pore opening. Understanding this P2X7R channel function is key for developing new anti-inflammatory and anticancer drugs.
Area of Science:
- Cell Biology
- Immunology
- Pharmacology
Background:
- Extracellular ATP acts as a damage-associated molecular pattern (DAMP), activating P2X7 receptors (P2X7Rs).
- P2X7Rs are ion channels involved in NLRP3 inflammasome activation and tumor cell growth.
- Overstimulation of P2X7Rs leads to a nonselective plasma membrane 'macropore' allowing large molecule flux.
Purpose of the Study:
- To investigate the molecular identity and function of the P2X7R-dependent conductance pathway.
- To elucidate the role of P2X7R-mediated plasma membrane permeability in pathophysiological processes.
- To provide a basis for developing novel anti-inflammatory and anticancer therapeutics targeting P2X7R.
Main Methods:
- Analysis of P2X7R channel properties and permeability.
- Investigating the relationship between P2X7R activation and plasma membrane changes.
- Reviewing recent reports on P2X7R solute permeability.
Main Results:
- Recent findings suggest P2X7R permeability to organic solutes is an intrinsic property of the channel.
- The molecular identity of the P2X7R-dependent pore remains unknown.
- P2X7R overstimulation opens a macropore allowing passage of large hydrophilic molecules.
Conclusions:
- Understanding P2X7R-dependent plasma membrane permeability changes is crucial.
- This knowledge can guide the rational development of novel anti-inflammatory and anticancer drugs targeting P2X7R pathways.
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