P2X4
Target has curated data in GtoImmuPdb
Target id: 481
Nomenclature: P2X4
Family: P2X receptors
Annotation status:
Awaiting annotation/under development. Please contact us if you can help with annotation.
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Contents:
Gene and Protein Information  |
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| Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
| Human | 2 | 388 | 12q24.32 | P2RX4 | purinergic receptor P2X 4 | 5 |
| Mouse | 2 | 388 | 5 F | P2rx4 | purinergic receptor P2X | 13 |
| Rat | 2 | 388 | 12q16 | P2rx4 | purinergic receptor P2X 4 | 1-2,11-13,15 |
| Previous and Unofficial Names |
| P2X purinoceptor 4 | purinergic receptor P2X, ligand-gated ion channel, 4 | purinergic receptor P2X, ligand gated ion channel, 4 | purinergic receptor P2X |
| Database Links |
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| CATH/Gene3D | 2.60.490.10 |
| ChEMBL Target | 10410 (Hs), 11949 (Rn) |
| Ensembl Gene | ENSG00000135124 (Hs), ENSMUSG00000029470 (Mm), ENSRNOG00000001300 (Rn) |
| Entrez Gene | 5025 (Hs), 18438 (Mm), 29659 (Rn) |
| Human Protein Atlas | ENSG00000135124 (Hs) |
| KEGG Gene | hsa:5025 (Hs), mmu:18438 (Mm), rno:29659 (Rn) |
| OMIM | 600846 (Hs) |
| RefSeq Nucleotide | NM_002560 (Hs), NM_011026 (Mm), NM_031594 (Rn) |
| RefSeq Protein | NP_002551 (Hs), NP_035156 (Mm), NP_113782 (Rn) |
| UniProtKB | Q99571 (Hs), Q9JJX6 (Mm), P51577 (Rn) |
| Wikipedia | P2RX4 (Hs) |
| Natural/Endogenous Ligands |
| ATP |
Download all structure-activity data for this target as a CSV file 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| View species-specific agonist tables | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Immunopharmacology Comments |
| P2X ligand-gated ion channels elicit pro-inflammatory immune responses upon activation by extracellular ATP that acts as a DAMP when released from damaged or infected cells [3-4]. |
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References
1. Bo X, Zhang Y, Nassar M, Burnstock G, Schoepfer R. (1995) A P2X purinoceptor cDNA conferring a novel pharmacological profile. FEBS Lett., 375 (1-2): 129-33. [PMID:7498461]
2. Buell G, Lewis C, Collo G, North RA, Surprenant A. (1996) An antagonist-insensitive P2X receptor expressed in epithelia and brain. EMBO J., 15 (1): 55-62. [PMID:8598206]
3. Burnstock G, Boeynaems JM. (2014) Purinergic signalling and immune cells. Purinergic Signal., 10 (4): 529-64. [PMID:25352330]
4. Cekic C, Linden J. (2016) Purinergic regulation of the immune system. Nat. Rev. Immunol., 16 (3): 177-92. [PMID:26922909]
5. Garcia-Guzman M, Soto F, Gomez-Hernandez JM, Lund PE, Stühmer W. (1997) Characterization of recombinant human P2X4 receptor reveals pharmacological differences to the rat homologue. Mol. Pharmacol., 51 (1): 109-18. [PMID:9016352]
6. Jacobson KA, Jarvis MF, Williams M. (2002) Purine and pyrimidine (P2) receptors as drug targets. J. Med. Chem., 45 (19): 4057-93. [PMID:12213051]
7. Jacobson KA, Müller CE. (2016) Medicinal chemistry of adenosine, P2Y and P2X receptors. Neuropharmacology, 104: 31-49. [PMID:26686393]
8. Khakh BS, Proctor WR, Dunwiddie TV, Labarca C, Lester HA. (1999) Allosteric control of gating and kinetics at P2X(4) receptor channels. J. Neurosci., 19 (17): 7289-99. [PMID:10460235]
9. North RA, Jarvis MF. (2013) P2X receptors as drug targets. Mol. Pharmacol., 83 (4): 759-69. [PMID:23253448]
10. Przybyła T, Sakowicz-Burkiewicz M, Pawełczyk T. (2018) Purinergic signaling in B cells. Acta Biochim. Pol., 65 (1): 1-7. [PMID:29360885]
11. Soto F, Garcia-Guzman M, Gomez-Hernandez JM, Hollmann M, Karschin C, Stühmer W. (1996) P2X4: an ATP-activated ionotropic receptor cloned from rat brain. Proc. Natl. Acad. Sci. U.S.A., 93 (8): 3684-8. [PMID:8622997]
12. Séguéla P, Haghighi A, Soghomonian JJ, Cooper E. (1996) A novel neuronal P2x ATP receptor ion channel with widespread distribution in the brain. J. Neurosci., 16 (2): 448-55. [PMID:8551329]
13. Townsend-Nicholson A, King BF, Wildman SS, Burnstock G. (1999) Molecular cloning, functional characterization and possible cooperativity between the murine P2X4 and P2X4a receptors. Brain Res. Mol. Brain Res., 64 (2): 246-54. [PMID:9931497]
14. Vaeth M, Feske S. (2018) Ion channelopathies of the immune system. Curr. Opin. Immunol., 52: 39-50. [PMID:29635109]
15. Wang CZ, Namba N, Gonoi T, Inagaki N, Seino S. (1996) Cloning and pharmacological characterization of a fourth P2X receptor subtype widely expressed in brain and peripheral tissues including various endocrine tissues. Biochem. Biophys. Res. Commun., 220 (1): 196-202. [PMID:8602843]
How to cite this page
Francesco Di Virgilio, Richard J. Evans, Simonetta Falzoni, Michael F. Jarvis, Charles Kennedy, Baljit S. Khakh, Brian King, Patrizia Pellegatti, John A. Peters.
P2X receptors: P2X4. Last modified on 13/09/2018. Accessed on 19/03/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=481.
