ArticleThe Journal of neuroscience : the official journal of the Society for Neuroscience2007
Thr339-to-serine substitution in rat P2X2 receptor second transmembrane domain causes constitutive opening and indicates a gating role for Lys308.
Article in The Journal of neuroscience : the official journal of the Society for Neuroscience, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed, 57 citations in OpenAlex.
- Channeling teamwork: ATP and lipids cooperate to gate P2X receptors.Science advances · 2026Review
- Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs.Science advances · 2026Article
- Mechanisms of ligand recognition and channel opening for P2X2 receptors in lipid nanodiscs.bioRxiv : the preprint server for biology · 2025Article
- Article
- Drosophila taste neurons as an agonist-screening platform for P2X receptors.Scientific reports · 2020Article
- Hearing loss mutations alter the functional properties of human P2X2 receptor channels through distinct mechanisms.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Mechanistic insights from resolving ligand-dependent kinetics of conformational changes at ATP-gated P2X1R ion channels.Scientific reports · 2016Article
- Photo-switchable tweezers illuminate pore-opening motions of an ATP-gated P2X ion channel.eLife · 2016Article
- Insights into the channel gating of P2X receptors from structures, dynamics and small molecules.Acta pharmacologica Sinica · 2016Review
- Key sites for P2X receptor function and multimerization: overview of mutagenesis studies on a structural basis.Current medicinal chemistry · 2015Review
- Signal transmission within the P2X2 trimeric receptor.The Journal of general physiology · 2014Article
- Direct gating of ATP-activated ion channels (P2X2 receptors) by lipophilic attachment at the outer end of the second transmembrane domain.The Journal of biological chemistry · 2014Article
- Exploring the ATP-binding site of P2X receptors.Frontiers in cellular neuroscience · 2013Review
- Optical control of an ion channel gate.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- P2X receptor intermediate activation states have altered nucleotide selectivity.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- P2X receptor chimeras highlight roles of the amino terminus to partial agonist efficacy, the carboxyl terminus to recovery from desensitization, and independent regulation of channel transitions.The Journal of biological chemistry · 2013Article
- P2X receptors as drug targets.Molecular pharmacology · 2013Review
- Insights into the Molecular Mechanisms Underlying Mammalian P2X7 Receptor Functions and Contributions in Diseases, Revealed by Structural Modeling and Single Nucleotide Polymorphisms.Frontiers in pharmacology · 2013Article
- Involvement of the cysteine-rich head domain in activation and desensitization of the P2X1 receptor.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Tightening of the ATP-binding sites induces the opening of P2X receptor channels.The EMBO journal · 2012Article
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
P2X2 receptors are ATP-gated ion channels widely expressed by neurons. Thr339 lies in the second of the two transmembrane domains of the rat P2X2 receptor protein, and is likely to be close to the narrowest part of the pore. Single-channel and whole-cell recording after expression in human embryonic kidney 293 cells showed that P2X2[T339S] receptors had pronounced spontaneous channel openings that were never seen in wild-type P2X2 receptors. P2X2[T339S] receptors were 10-fold more sensitive than wild type to exogenous ATP, and alphabeta meATP also increased channel opening. Two conserved ectodomain lysine residues (Lys69 and Lys308) are critical for function and have been proposed to contribute to the ATP binding site of P2X receptors. The spontaneous opening of P2X2[K69A/T339S] receptors was not different than that seen in P2X2[T339S], but for P2X2[K308A/T339S] the spontaneous activity was absent. Suramin, which is a noncompetitive antagonist at wild-type P2X2 receptors, had a pronounced agonist action at both P2X2[T339S] and P2X2[K69A/T339S] receptors but not at P2X2[K308A/T339S]. 2',3'-O-O-(2,4,6-Trinitrophenyl)-ATP (TNP-ATP), which is a competitive agonist at wild-type receptors, was also an agonist at P2X2[T339S] receptors, but not at either double mutant. The results indicate that the T339S mutation substantially destabilizes the closed channel and suggest an important role in channel gating. The correction of this gating defect, in the absence of any agonist, by the second mutation K308A shows that Lys308 is also involved in channel gating. A similar interpretation can account for the results with suramin and TNP-ATP.
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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.