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

Illes, Peter; Mueller, Christa E; Jacobson, Kenneth A; Grutter, Thomas; Nicke, Annette; Fountain, Samuel J; Kennedy, Charles; ... Di Virgilio, Francesco; + view all (2021) Update of P2X receptor properties and their pharmacology: IUPHAR Review 30. British Journal of Pharmacology , 178 (3) pp. 489-514. 10.1111/bph.15299. Green open access

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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).

Type: Article
Title: Update of P2X receptor properties and their pharmacology: IUPHAR Review 30
Location: England
Open access status: An open access version is available from UCL Discovery
DOI: 10.1111/bph.15299
Publisher version: https://doi.org/10.1111/bph.15299
Language: English
Additional information: © 2020 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
Keywords: Science & Technology, Life Sciences & Biomedicine, Pharmacology & Pharmacy, (patho)physiological functions, agonists, antagonists, extracellular ATP, knockout mice, ligand&#8208, gated cationic channels, P2X receptors, ATP-GATED P2X, ION-CHANNEL, ALLOSTERIC MODULATION, MEDICINAL CHEMISTRY, CONCISE GUIDE, FUNCTIONAL-PROPERTIES, INTERNATIONAL UNION, PURINERGIC RECEPTOR, EXTRACELLULAR ATP, KNOCKOUT MICE
UCL classification: UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Life Sciences > Div of Biosciences > Neuro, Physiology and Pharmacology
URI: https://discovery.ucl.ac.uk/id/eprint/10164310
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