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P2X5

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Target id: 482

Nomenclature: P2X5

Family: P2X receptors

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 444 17p13.2 P2RX5 purinergic receptor P2X 5 3,10-11
Mouse 2 455 11 B4 P2rx5 purinergic receptor P2X, ligand-gated ion channel, 5 7
Rat 2 455 10q24 P2rx5 purinergic receptor P2X 5 6
Gene and Protein Information Comments
Seventy-five P2X5 genes have been identified in the genomes of 75 placental mammalian species (Eutheria) [14].
Previous and Unofficial Names Click here for help
P2X purinoceptor 5 | purinergic receptor P2X, ligand gated ion channel, 5 | purinergic receptor P2X
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands Click here for help
ATP
Comments: Endogenous agonist: ATP at human [3] and mouse [7] P2X5 receptors.

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
ATP Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Ligand has a PDB structure Rn Agonist 6.0 pEC50 8
pEC50 6.0 (EC50 1x10-6 M) [8]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
suramin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Rn Antagonist 5.4 pIC50 8
pIC50 5.4 (IC50 4x10-6 M) [8]
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 [4-5].
Cell Type Associations
Immuno Cell Type:  B cells
Cell Ontology Term:   B cell (CL:0000236)
Comment:  Human B cells express all P2 receptor subtypes.
References:  12
Immuno Cell Type:  T cells
Comment:  T cells express P2X receptors 1, 4 and 5. ATP-induced activation of these receptors in T cells is associated with proliferation, cytokine production and thymocyte apoptosis.
References:  5,13
Immuno Process Associations
Immuno Process:  Tissue repair
GO Annotations:  Associated to 1 GO processes
GO:0043416 regulation of skeletal muscle tissue regeneration ISO
Physiological Consequences of Altering Gene Expression Click here for help
Altered inflammatory response in murine osteoclasts, with reduced bone loss.
Species:  Mouse
Tissue:  Osteoclasts
Technique:  Gene knockout
References:  9
General Comments
The human P2X5 subunit exists as 3 alternatively spliced isoforms (A, which is tabulated above; B, NP_778255 - 397 aa and C, NP_778256 - 178 aa).

Of all the functional P2X receptors, only P2X5 homopolymer is unregulated by intracellular PIPn [1-2].

References

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1. Ase AR, Bernier LP, Blais D, Pankratov Y, Séguéla P. (2010) Modulation of heteromeric P2X1/5 receptors by phosphoinositides in astrocytes depends on the P2X1 subunit. J. Neurochem., 113 (6): 1676-84. [PMID:20374427]

2. Bernier LP, Ase AR, Séguéla P. (2013) Post-translational regulation of P2X receptor channels: modulation by phospholipids. Front Cell Neurosci, 7: 226. [PMID:24324400]

3. Bo X, Jiang LH, Wilson HL, Kim M, Burnstock G, Surprenant A, North RA. (2003) Pharmacological and biophysical properties of the human P2X5 receptor. Mol. Pharmacol., 63 (6): 1407-16. [PMID:12761352]

4. Burnstock G, Boeynaems JM. (2014) Purinergic signalling and immune cells. Purinergic Signal., 10 (4): 529-64. [PMID:25352330]

5. Cekic C, Linden J. (2016) Purinergic regulation of the immune system. Nat. Rev. Immunol., 16 (3): 177-92. [PMID:26922909]

6. Collo G, North RA, Kawashima E, Merlo-Pich E, Neidhart S, Surprenant A, Buell G. (1996) Cloning OF P2X5 and P2X6 receptors and the distribution and properties of an extended family of ATP-gated ion channels. J. Neurosci., 16 (8): 2495-507. [PMID:8786426]

7. Cox JA, Barmina O, Voigt MM. (2001) Gene structure, chromosomal localization, cDNA cloning and expression of the mouse ATP-gated ionotropic receptor P2X5 subunit. Gene, 270 (1-2): 145-52. [PMID:11404011]

8. Jacobson KA, Jarvis MF, Williams M. (2002) Purine and pyrimidine (P2) receptors as drug targets. J. Med. Chem., 45 (19): 4057-93. [PMID:12213051]

9. Kim H, Walsh MC, Takegahara N, Middleton SA, Shin HI, Kim J, Choi Y. (2017) The purinergic receptor P2X5 regulates inflammasome activity and hyper-multinucleation of murine osteoclasts. Sci Rep, 7 (1): 196. [PMID:28298636]

10. Kotnis S, Bingham B, Vasilyev DV, Miller SW, Bai Y, Yeola S, Chanda PK, Bowlby MR, Kaftan EJ, Samad TA et al.. (2010) Genetic and functional analysis of human P2X5 reveals a distinct pattern of exon 10 polymorphism with predominant expression of the nonfunctional receptor isoform. Mol Pharmacol, 77 (6): 953-60. [PMID:20223879]

11. Lê KT, Paquet M, Nouel D, Babinski K, Séguéla P. (1997) Primary structure and expression of a naturally truncated human P2X ATP receptor subunit from brain and immune system. FEBS Lett., 418 (1-2): 195-9. [PMID:9414125]

12. Przybyła T, Sakowicz-Burkiewicz M, Pawełczyk T. (2018) Purinergic signaling in B cells. Acta Biochim. Pol., 65 (1): 1-7. [PMID:29360885]

13. Vaeth M, Feske S. (2018) Ion channelopathies of the immune system. Curr. Opin. Immunol., 52: 39-50. [PMID:29635109]

14. Zdobnov EM, Tegenfeldt F, Kuznetsov D, Waterhouse RM, Simão FA, Ioannidis P, Seppey M, Loetscher A, Kriventseva EV. (2017) OrthoDB v9.1: cataloging evolutionary and functional annotations for animal, fungal, plant, archaeal, bacterial and viral orthologs. Nucleic Acids Res., 45 (D1): D744-D749. [PMID:27899580]

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