ArticleNature structural & molecular biology2008
Mapping a molecular link between allosteric inhibition and activation of the glycine receptor.
Article in Nature structural & molecular biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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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
22 citing papers in PubMed.
- Structural basis for domain coupling in heteromeric glycine receptors revealed by an atypical allosteric agonist.Science advances · 2026Article
- Discovering cryptic pocket opening and binding of a stimulant derivative in a vestibular site of the 5-HTScience advances · 2025Article
- Exploring the Activation Process of the Glycine Receptor.Journal of the American Chemical Society · 2024Article
- Ancestral acetylcholine receptor β-subunit forms homopentamers that prime before opening spontaneously.eLife · 2022Article
- Modulation of theeLife · 2020Article
- Disruption of a putative intersubunit electrostatic bond enhances agonist efficacy at the human α1 glycine receptor.Brain research · 2017Article
- Structure and Pharmacologic Modulation of Inhibitory Glycine Receptors.Molecular pharmacology · 2016Review
- Murine startle mutant Nmf11 affects the structural stability of the glycine receptor and increases deactivation.The Journal of physiology · 2016Article
- Ethanol effects on glycinergic transmission: From molecular pharmacology to behavior responses.Pharmacological research · 2015Review
- Glycine receptor mouse mutants: model systems for human hyperekplexia.British journal of pharmacology · 2013Review
- Inhibitory glycine receptors: an update.The Journal of biological chemistry · 2012Review
- Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site.The Journal of biological chemistry · 2012Article
- Synaptic neurotransmitter-gated receptors.Cold Spring Harbor perspectives in biology · 2012Review
- Structural link between γ-aminobutyric acid type A (GABAA) receptor agonist binding site and inner β-sheet governs channel activation and allosteric drug modulation.The Journal of biological chemistry · 2012Article
- Packing of the extracellular domain hydrophobic core has evolved to facilitate pentameric ligand-gated ion channel function.The Journal of biological chemistry · 2011Article
- Molecular sites for the positive allosteric modulation of glycine receptors by endocannabinoids.PloS one · 2011Article
- Pulsed electron spin resonance resolves the coordination site of Cu²(+) ions in α1-glycine receptor.Biophysical journal · 2010Article
- Ethanol enhances taurine-activated glycine receptor function.Alcoholism, clinical and experimental research · 2010Article
- Probing pore constriction in a ligand-gated ion channel by trapping a metal ion in the pore upon agonist dissociation.The Journal of biological chemistry · 2010Article
- Pathophysiological mechanisms of dominant and recessive GLRA1 mutations in hyperekplexia.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2010Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
Cys-loop ligand-gated ion channels mediate rapid neurotransmission throughout the central nervous system. They possess agonist recognition sites and allosteric sites where modulators regulate ion channel function. Using strychnine-sensitive glycine receptors, we identified a scaffold of hydrophobic residues enabling allosteric communication between glycine-agonist binding loops A and D, and the Zn(2+)-inhibition site. Mutating these hydrophobic residues disrupted Zn(2+) inhibition, generating novel Zn(2+)-activated receptors and spontaneous channel activity. Homology modeling and electrophysiology revealed that these phenomena are caused by disruption to three residues on the '-' loop face of the Zn(2+)-inhibition site, and to D84 and D86, on a neighboring beta3 strand, forming a Zn(2+)-activation site. We provide a new view for the activation of a Cys-loop receptor where, following agonist binding, the hydrophobic core and interfacial loops reorganize in a concerted fashion to induce downstream gating.
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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.