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Purinergic P2X receptors: Structural and functional features depicted by X-ray and molecular modelling studies

Grimes, Leanne and Young, Mark ORCID: 2015. Purinergic P2X receptors: Structural and functional features depicted by X-ray and molecular modelling studies. Current Medicinal Chemistry 22 (7) , pp. 783-798. 10.2174/0929867321999141212131457

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The publication of the first crystal structures of the zebrafish P2X4 receptor in 2009 was a pivotal moment; for the first time, researchers were able to interpret their experimental data in a structural context. Several research groups immediately set about using the data to make molecular models of the betterunderstood mammalian P2X receptors, in order to design and interpret the results of new, more focused structure- function experiments. In 2012, the publication of the crystal structure of zebrafish P2X4 in the ATPbound state gave further insights into the mechanism of ligand binding and its coupling to ion channel activation, initiating a new cycle of modelling, experimentation and interpretation. The purpose of this review is to describe our current understanding of the 3D-structure of P2X receptors, by highlighting the strengths and limitations of the zebrafish P2X4 crystal structures, discussing how the molecular models derived from them have been made, and what they have been used for, and explaining why crystal structures of mammalian P2X receptors are still needed to uncover the molecular mechanisms of differential agonist/antagonist potency, allosteric modulation, pore dilatation and desensitisation.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > QR Microbiology
Uncontrolled Keywords: Crystal structure; P2X; molecular dynamics; molecular modelling; structure-function
Publisher: Bentham Science Publishers
ISSN: 0929-8673
Date of First Compliant Deposit: 30 March 2016
Last Modified: 12 Nov 2023 20:25

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