Purinergic Receptor P2X Ligand-Gated Ion Channel 7
| P2X7 (P2X7R) | |
|---|---|
| Gene | [P2RX7](/genes/p2rx7) |
| UniProt ID | [Q99572](https://www.uniprot.org/uniprot/Q99572) |
| PDB Structures | 5U1W, 6U9V, 7R0F |
| Molecular Weight | 68.5 kDa |
| Subcellular Localization | Plasma membrane, microglial cells, immune cells |
| Protein Family | |
| P2X receptor family (ATP-gated ion channel) | |
| Function | ATP-gated ion channel, inflammasome activation |
P2X7 Protein is a protein. This page describes its structure, normal nervous system function, role in neurodegenerative disease, and potential as a therapeutic target.
P2X7 is a member of the P2X receptor family, which are ATP-gated non-selective cation channels[1]. The receptor contains:
P2X7 can form both homomeric and heteromeric channels with other P2X subunits.
P2X7 receptors play important roles in neuroimmune signaling:
P2X7 is upregulated in microglia surrounding amyloid plaques[3]. The receptor contributes to neuroinflammation through NLRP3 inflammasome activation. Genetic variants of P2X7 are associated with AD risk.
P2X7 on microglia mediates dopaminergic neuron loss. Blocking P2X7 provides neuroprotection in PD models.
P2X7 contributes to neuroinflammation in ALS. Microglial P2X7 activation leads to motor neuron damage.
P2X7 drives inflammatory responses in microglia and astrocytes. The receptor is a therapeutic target.
| Compound | Status | Mechanism |
|---|---|---|
| Brilliant Blue G | Preclinical | P2X7 antagonist |
| AZD9056 | Clinical Trial | P2X7 antagonist (rheumatoid arthritis) |
| CE-224535 | Clinical Trial | P2X7 antagonist (PD) |
Hattori M, Gouaux E. Molecular mechanism of ATP binding and ion channel activation in P2X7 receptors. Nature. 2012. ↩︎
Burnstock G. Purinergic signaling in the nervous system. Nat Rev Neurosci. 2009. ↩︎
Bhattacharya A, et al. P2X7 receptors: role in amyloid-β pathology. J Neurosci. 2014. ↩︎