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P2X6

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 483

Nomenclature: P2X6

Family: P2X receptors

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 441 22q11.21 P2RX6 purinergic receptor P2X 6 11
Mouse 2 389 16 A3 P2rx6 purinergic receptor P2X, ligand-gated ion channel, 6 8
Rat 2 389 11q23 P2rx6 purinergic receptor P2X 6 3
Gene and Protein Information Comments
Seventy-four P2X6 genes have been identified in the genomes of 71 placental mammalian species (Eutheria). (Multi-copies in two species) [12].
Previous and Unofficial Names Click here for help
P2RXL1 | P2XM | P2X purinoceptor 6 | P2X6 receptor | purinergic receptor P2X-like 1 orphan receptor | Rnap2x6 | RNRNAP2X6 | purinergic receptor P2X, ligand-gated ion channel, 6 | purinergic receptor P2X, ligand gated ion channel, 6 | 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

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Agonists
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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 5
pEC50 6.0 (EC50 1x10-6 M) [5]
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 [1-2].
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:  9
Physiological Consequences of Altering Gene Expression Click here for help
Compensatory upregulation of P2X2 in heart.
Species:  Mouse
Tissue:  Whole animal
Technique:  Gene knockout
References:  4
General Comments
P2X6 is largely retained in the endoplasmic reticulum and fails to exit as a homopolymer, although it may do as a heteropolymer (with P2X2 or P2X4, and with both). However, enhanced glycosylation of P2X6 may improve trafficking of P2X6 homopolymers and can result in functional ATP-activated receptors [6-7,10].

References

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

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

3. 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]

4. de Baaij JH, Kompatscher A, Viering DH, Bos C, Bindels RJ, Hoenderop JG. (2016) P2X6 Knockout Mice Exhibit Normal Electrolyte Homeostasis. PLoS ONE, 11 (6): e0156803. [PMID:27254077]

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

6. Jones CA, Vial C, Sellers LA, Humphrey PP, Evans RJ, Chessell IP. (2004) Functional regulation of P2X6 receptors by N-linked glycosylation: identification of a novel alpha beta-methylene ATP-sensitive phenotype. Mol. Pharmacol., 65 (4): 979-85. [PMID:15044628]

7. Kaczmarek-Hájek K, Lörinczi E, Hausmann R, Nicke A. (2012) Molecular and functional properties of P2X receptors--recent progress and persisting challenges. Purinergic Signal., 8 (3): 375-417. [PMID:22547202]

8. Nawa G, Urano T, Tokino T, Ochi T, Miyoshi Y. (1998) Cloning and characterization of the murine P2XM receptor gene. J. Hum. Genet., 43 (4): 262-7. [PMID:9852680]

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

10. Robinson LE, Murrell-Lagnado RD. (2013) The trafficking and targeting of P2X receptors. Front Cell Neurosci, 7: 233. [PMID:24319412]

11. Urano T, Nishimori H, Han H, Furuhata T, Kimura Y, Nakamura Y, Tokino T. (1997) Cloning of P2XM, a novel human P2X receptor gene regulated by p53. Cancer Res., 57 (15): 3281-7. [PMID:9242461]

12. 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]

Contributors

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