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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 2 | 595 | 12q24.31 | P2RX7 | purinergic receptor P2X 7 | 15,80 |
Mouse | 2 | 595 | 5 F | P2rx7 | purinergic receptor P2X, ligand-gated ion channel, 7 | 20 |
Rat | 2 | 595 | 12q16 | P2rx7 | purinergic receptor P2X 7 | 95 |
Previous and Unofficial Names |
P2X purinoceptor 7 | P2Z receptor | P2X7 receptor | purinergic receptor P2X, ligand gated ion channel, 7 | purinergic receptor P2X |
Database Links | |
Alphafold | Q99572 (Hs), Q9Z1M0 (Mm), Q64663 (Rn) |
CATH/Gene3D | 2.60.490.10 |
ChEMBL Target | CHEMBL4805 (Hs), CHEMBL5183 (Mm), CHEMBL2496 (Rn) |
Ensembl Gene | ENSG00000089041 (Hs), ENSMUSG00000029468 (Mm), ENSRNOG00000001296 (Rn) |
Entrez Gene | 5027 (Hs), 18439 (Mm), 29665 (Rn) |
Human Protein Atlas | ENSG00000089041 (Hs) |
KEGG Gene | hsa:5027 (Hs), mmu:18439 (Mm), rno:29665 (Rn) |
OMIM | 602566 (Hs) |
Pharos | Q99572 (Hs) |
RefSeq Nucleotide | NM_002562 (Hs), NM_001284402 (Mm), NM_011027 (Mm), NM_019256 (Rn) |
RefSeq Protein | NP_002553 (Hs), NP_035157 (Mm), NP_001271331 (Mm), NP_062129 (Rn) |
UniProtKB | Q99572 (Hs), Q9Z1M0 (Mm), Q64663 (Rn) |
Wikipedia | P2RX7 (Hs) |
Natural/Endogenous Ligands |
ATP |
Download all structure-activity data for this target as a CSV file
Agonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific agonist tables |
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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View species-specific antagonist tables | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Antagonist Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Oxidized ATP is an irreversible antagonist of P2X7 [70]. |
Allosteric Modulators | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Allosteric Modulator Comments | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Effects of the allosteric regulators at P2X7 receptors are species-dependent. See Michel et al. (2008) [67] for an explanation. No affinity data has been published quantifying the complex interaction of GW791343 with the P2X7 receptor. We have included the interaction in the table above based on extensive experimental evidence provided in [66] and [67]. Polymyxin B is a P2X7 receptor PAM [37]. |
Immunopharmacology Comments |
The P2X7 receptor is involved in NLRP3-type inflammasome formation, and subsequent maturation of IL-1β [63,81]. In human mast cells P2X7 receptor activation causes degranulation and inflammatory mediator release [102], and in mouse mast cells induces IL-6 and TNF-α production [63]. Studies in mice suggest that ATP released from damaged airway tissue engages the P2X7 receptor/pannexin-1 axis, leading to IL-1β maturation and pulmonary fibrosis.[82]. P2X7 receptor antagonism has also been posited as a potential pharmaceutical intervention to treat the salivary gland inflammation and sequelae of Sjögrens syndrome [60]. |
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General Comments |
The role of P2X7 receptor in cancer is discussed in [25-27]. The crystal structure of the truncated (lacking 240 C-terminal residues) P2X7 receptor from giant panda (Ailuropoda melanoleuca) has been resolved. This has allowed identification of the mechanism of action of several widely used antagonists [56]. Recent crystallographic data suggest that three antagonists (A740003, A804598, JNJ-47965567) previously classified as competitive inhibitors are in fact allosteric, non competitive, inhibitors [56]. |
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37. Ferrari D, Pizzirani C, Adinolfi E, Forchap S, Sitta B, Turchet L, Falzoni S, Minelli M, Baricordi R, Di Virgilio F. (2004) The antibiotic polymyxin B modulates P2X7 receptor function. J Immunol, 173 (7): 4652-60. [PMID:15383600]
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