Top ▲


Click here for help

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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
Natural/Endogenous Ligands Click here for help

Download all structure-activity data for this target as a CSV file go icon to follow link

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 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].


Show »

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]


Show »

How to cite this page