Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

Illes, Peter, Müller, Christa E., Jacobson, Kenneth A., Grutter, Thomas, Nicke, Annette, Fountain, Samuel J., Kennedy, Charles, Schmalzing, Günther, Jarvis, Michael F., Stojilkovic, Stanko S., King, Brian F. and Di Virgilio, Francesco (2021) Update of P2X receptor properties and their pharmacology: IUPHAR Review 30. British Journal of Pharmacology, 178 (3). pp. 489-514. ISSN 0007-1188

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Abstract

The known seven mammalian receptor subunits (P2X1–7) form cationic channels gated by ATP. Three subunits compose a receptor channel. Each subunit is a polypeptide consisting of two transmembrane regions (TM1 and TM2), intracellular N- and C-termini, and a bulky extracellular loop. Crystallization allowed the identification of the 3D structure and gating cycle of P2X receptors. The agonist-binding pocket is located at the intersection of two neighbouring subunits. In addition to the mammalian P2X receptors, their primitive ligand-gated counterparts with little structural similarity have also been cloned. Selective agonists for P2X receptor subtypes are not available, but medicinal chemistry supplied a range of subtype-selective antagonists, as well as positive and negative allosteric modulators. Knockout mice and selective antagonists helped to identify pathological functions due to defective P2X receptors, such as male infertility (P2X1), hearing loss (P2X2), pain/cough (P2X3), neuropathic pain (P2X4), inflammatory bone loss (P2X5), and faulty immune reactions (P2X7).

Item Type: Article
Additional Information: This article is protected by copyright. All rights reserved.
Uncontrolled Keywords: (patho)physiological functions,p2x receptors,agonists,antagonists,extracellular atp,knockout mice,ligand-gated cationic channels,pharmacology ,/dk/atira/pure/subjectarea/asjc/3000/3004
Faculty \ School: Faculty of Science
Faculty of Medicine and Health Sciences > Norwich Medical School
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Depositing User: LivePure Connector
Date Deposited: 03 Nov 2020 11:49
Last Modified: 13 May 2021 15:41
URI: https://ueaeprints.uea.ac.uk/id/eprint/77518
DOI: 10.1111/bph.15299

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