P2X7 receptors: channels, pores and more
C Volonté1, S Apolloni, S D Skaper
1Cell Biology and Neurobiology Institute, CNR/FSL, Via del Fosso di Fiorano 65, 00143 Rome, Italy. cinzia.volonte@cnr.it
CNS & Neurological Disorders Drug Targets
|September 12, 2012
Summary
The P2X7 receptor (P2X7R) acts as a crucial link between the nervous and immune systems. Its role in inflammation and cytokine release suggests therapeutic potential for neurological and psychiatric disorders.
Area of Science:
- Neuroscience
- Immunology
- Pharmacology
Background:
- Purine nucleotides, like ATP, are extracellular signals.
- P2X7 receptors (P2X7Rs) are ATP-gated ion channels found on immune cells.
- P2X7Rs mediate cation influx and pro-inflammatory cytokine release.
Purpose of the Study:
- To review the biology and pharmacology of P2X7Rs.
- To explore the role of P2X7Rs in neurological and psychiatric diseases.
- To highlight P2X7R as a potential therapeutic target.
Main Methods:
- Literature review of P2X7R function and disease association.
- Analysis of P2X7R's role in cytokine regulation and cell death.
- Examination of genetic polymorphisms affecting P2X7R function.
Main Results:
- P2X7Rs have a bifunctional nature, opening small cation channels and larger pores.
- Genetic variations in P2RX7 impact receptor function.
- P2X7R activation promotes inflammation and cytokine release, implicated in neurodegeneration and pain.
Conclusions:
- P2X7Rs are key mediators of inflammatory and immune responses.
- Dysregulation of P2X7R is linked to neurological and psychiatric disorders.
- Targeting P2X7R offers therapeutic possibilities for these conditions.
Related Concept Videos
Mechanically-gated Ion Channels
Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
Mechanically-gated Ion Channels
Mechanically-gated ion channels are proteins found in eukaryotic and prokaryotic cell membranes that open in response to mechanical stress. Tension, compression, swelling, and shear stress can alter the conformation of the protein, opening a transmembrane channel that allows the passage of ions for signal transmission. In eukaryotes, mechanically-gated channels are distributed in several regions like the neurons, lungs, skin, bladder, and heart, where they play critical roles in numerous...
Ligand-gated Ion Channels
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Ligand-gated Ion Channels
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that include the...
Non-gated Ion Channels
Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Non-gated Ion Channels
Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.

