9b73

Structural highlights

Function

P2RX1_HUMAN ATP-gated nonselective transmembrane cation channel permeable to potassium, sodium and with relatively high calcium permeability (PubMed:10440098, PubMed:15056721, PubMed:20699225, PubMed:8834001, PubMed:8961184). Furthermore, CTP functions as a weak affinity agonist for P2RX1 (PubMed:14699168). Plays a role a role in urogenital, immune and cardiovascular function (By similarity). Specifically, plays an important role in neurogenic contraction of smooth muscle of the vas deferens, and therefore is essential for normal male reproductive function (By similarity). In addition, contributes to smooth muscle contractions of the urinary bladder (By similarity). On platelets, contributes to platelet activation and aggregation and thereby, also to thrombosis (By similarity). On neutrophils, it is involved in chemotaxis and in mitigating the activation of circulating cells (PubMed:19635923).[UniProtKB:P51576]^{[1] [2] [3] [4] [5] [6] [7]}

References

1. ↑ Bianchi BR, Lynch KJ, Touma E, Niforatos W, Burgard EC, Alexander KM, Park HS, Yu H, Metzger R, Kowaluk E, Jarvis MF, van Biesen T. Pharmacological characterization of recombinant human and rat P2X receptor subtypes. Eur J Pharmacol. 1999 Jul 2;376(1-2):127-38. PMID:10440098 doi:10.1016/s0014-2999(99)00350-7
2. ↑ Roberts JA, Evans RJ. ATP binding at human P2X1 receptors. Contribution of aromatic and basic amino acids revealed using mutagenesis and partial agonists. J Biol Chem. 2004 Mar 5;279(10):9043-55. PMID:14699168 doi:10.1074/jbc.M308964200
3. ↑ Egan TM, Khakh BS. Contribution of calcium ions to P2X channel responses. J Neurosci. 2004 Mar 31;24(13):3413-20. PMID:15056721 doi:10.1523/JNEUROSCI.5429-03.2004
4. ↑ Lecut C, Frederix K, Johnson DM, Deroanne C, Thiry M, Faccinetto C, Marée R, Evans RJ, Volders PG, Bours V, Oury C. P2X1 ion channels promote neutrophil chemotaxis through Rho kinase activation. J Immunol. 2009 Aug 15;183(4):2801-9. PMID:19635923 doi:10.4049/jimmunol.0804007
5. ↑ Allsopp RC, Lalo U, Evans RJ. Lipid raft association and cholesterol sensitivity of P2X1-4 receptors for ATP: chimeras and point mutants identify intracellular amino-terminal residues involved in lipid regulation of P2X1 receptors. J Biol Chem. 2010 Oct 22;285(43):32770-32777. PMID:20699225 doi:10.1074/jbc.M110.148940
6. ↑ Valera S, Talabot F, Evans RJ, Gos A, Antonarakis SE, Morris MA, Buell GN. Characterization and chromosomal localization of a human P2X receptor from the urinary bladder. Recept Channels. 1995;3(4):283-9 PMID:8834001
7. ↑ Evans RJ, Lewis C, Virginio C, Lundstrom K, Buell G, Surprenant A, North RA. Ionic permeability of, and divalent cation effects on, two ATP-gated cation channels (P2X receptors) expressed in mammalian cells. J Physiol. 1996 Dec 1;497 ( Pt 2)(Pt 2):413-22. PMID:8961184 doi:10.1113/jphysiol.1996.sp021777