ArticleThe EMBO journal2012
Tightening of the ATP-binding sites induces the opening of P2X receptor channels.
Article in The EMBO journal, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 82 citations in OpenAlex.
- Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs.Science advances · 2026Article
- Mechanistic insights into ligand selectivity inActa pharmaceutica Sinica. B · 2026Article
- Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs.bioRxiv : the preprint server for biology · 2025Article
- Species Differences of P2X4 Receptor Modulators.ACS pharmacology & translational science · 2025Article
- A shared mechanism for TNP-ATP recognition by members of the P2X receptor family.Computational and structural biotechnology journal · 2024Article
- High-affinity agonism at the P2XNature communications · 2024Article
- Chronic cough relief by allosteric modulation of P2X3 without taste disturbance.Nature communications · 2023Article
- P2X2 receptor subunit interfaces are missense variant hotspots, where mutations tend to increase apparent ATP affinity.British journal of pharmacology · 2022Article
- How Structural Biology Has Directly Impacted Our Understanding of P2X Receptor Function and Gating.Methods in molecular biology (Clifton, N.J.) · 2022Article
- Molecular Pharmacology of P2X Receptors: Exploring Druggable Domains Revealed by Structural Biology.Frontiers in pharmacology · 2022Review
- Pathophysiological Role of Purinergic P2X Receptors in Digestive System Diseases.Frontiers in physiology · 2021Review
- Article
- Bile acids are potent inhibitors of rat P2X2 receptors.Purinergic signalling · 2019Article
- Druggable negative allosteric site of P2X3 receptors.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- The effect of sinomenine in diabetic neuropathic pain mediated by the P2XPurinergic signalling · 2017Article
- Intersubunit physical couplings fostered by the left flipper domain facilitate channel opening of P2X4 receptors.The Journal of biological chemistry · 2017Article
- P2X2 Dominant Deafness Mutations Have No Negative Effect on Wild-Type Isoform: Implications for Functional Rescue and in Deafness Mechanism.Frontiers in molecular neuroscience · 2017Article
- The Dynamic Behavior of the P2XBiophysical journal · 2016Article
- Article
- Inter-subunit disulfide locking of the human P2X3 receptor elucidates ectodomain movements associated with channel gating.Purinergic signalling · 2016Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The opening of ligand-gated ion channels in response to agonist binding is a fundamental process in biology. In ATP-gated P2X receptors, little is known about the molecular events that couple ATP binding to channel opening. In this paper, we identify structural changes of the ATP site accompanying the P2X2 receptor activation by engineering extracellular zinc bridges at putative mobile regions as revealed by normal mode analysis. We provide evidence that tightening of the ATP sites shaped like open 'jaws' induces opening of the P2X ion channel. We show that ATP binding favours jaw tightening, whereas binding of a competitive antagonist prevents gating induced by this movement. Our data reveal the inherent dynamic of the binding jaw, and provide new structural insights into the mechanism of P2X receptor activation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.