ArticleThe Journal of biological chemistry2012
Structural link between γ-aminobutyric acid type A (GABAA) receptor agonist binding site and inner β-sheet governs channel activation and allosteric drug modulation.
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 25 citations in OpenAlex.
- A pore-facing glycan constrains GABACommunications biology · 2026Article
- Introducing a proline in the α1 M2-M3 linker relieves a molecular brake on channel activation in α1β2γ2 GABAbioRxiv : the preprint server for biology · 2026Article
- Introducing a proline in the α1 M2-M3 linker relieves a molecular brake on channel activation in α1β2γ2 GABAA receptors.PloS one · 2026Article
- A Pore-Facing Glycan Determines GABAA Receptor Subunit Stoichiometry and Gating Behavior.Research square · 2025Article
- Ketamine in Status Epilepticus: How Soon Is Now?Neurology international · 2025Review
- Early Polytherapy for Probably Benzodiazepine Refractory Naïve Status Epilepticus (Stage 1 Plus).Neurology international · 2025Review
- GABABiophysical journal · 2024Article
- In the fast lane: Receptor trafficking during status epilepticus.Epilepsia open · 2023Review
- Article
- Benzodiazepine Modulation of GABABiomolecules · 2022Review
- A critical residue in the αeLife · 2021Article
- Modulation of theeLife · 2020Article
- 2-(4-methyl-thiazol-5-yl) ethyl nitrate maleate-potentiated GABACNS neuroscience & therapeutics · 2018Article
- An intersubunit electrostatic interaction in the GABAThe Journal of biological chemistry · 2018Article
- GABAScientific reports · 2017Article
- De novo GABRG2 mutations associated with epileptic encephalopathies.Brain : a journal of neurology · 2017Article
- Epileptic encephalopathy de novo GABRB mutations impair γ-aminobutyric acid type A receptor function.Annals of neurology · 2016Article
- Article
- Seeking potential anticonvulsant agents that target GABAA receptors using experimental and theoretical procedures.Journal of computer-aided molecular design · 2014Article
- Signal transmission within the P2X2 trimeric receptor.The Journal of general physiology · 2014Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Rapid opening and closing of pentameric ligand-gated ion channels (pLGICs) regulate information flow throughout the brain. For pLGICs, it is postulated that neurotransmitter-induced movements in the extracellular inner β-sheet trigger channel activation. Homology modeling reveals that the β4-β5 linker physically connects the neurotransmitter binding site to the inner β-sheet. Inserting 1, 2, 4, and 8 glycines in this region of the GABA(A) receptor β-subunit progressively decreases GABA activation and converts the competitive antagonist SR-95531 into a partial agonist, demonstrating that this linker is a key element whose length and flexibility are optimized for efficient signal propagation. Insertions in the α- and γ-subunits have little effect on GABA or SR-95531 actions, suggesting that asymmetric motions in the extracellular domain power pLGIC gating. The effects of insertions on allosteric modulator actions, pentobarbital, and benzodiazepines, have different subunit dependences, indicating that modulator-induced signaling is distinct from agonist gating.
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What OpenQuestion holds
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.