ArticleProceedings of the National Academy of Sciences of the United States of America2010
Disruption of an intersubunit electrostatic bond is a critical step in glycine receptor activation.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 16 citations in OpenAlex.
- Article
- An intersubunit electrostatic interaction in the GABAThe Journal of biological chemistry · 2018Article
- Disruption of a putative intersubunit electrostatic bond enhances agonist efficacy at the human α1 glycine receptor.Brain research · 2017Article
- Genetic and functional analyses demonstrate a role for abnormal glycinergic signaling in autism.Molecular psychiatry · 2016Article
- Intersubunit conformational changes mediate epithelial sodium channel gating.The Journal of general physiology · 2014Article
- Propofol modulation of α1 glycine receptors does not require a structural transition at adjacent subunits that is crucial to agonist-induced activation.ACS chemical neuroscience · 2013Article
- Glycine receptor mouse mutants: model systems for human hyperekplexia.British journal of pharmacology · 2013Review
- Synaptic neurotransmitter-gated receptors.Cold Spring Harbor perspectives in biology · 2012Review
- Isoflurane alters the structure and dynamics of GLIC.Biophysical journal · 2011Article
- Alcohol-binding sites in distinct brain proteins: the quest for atomic level resolution.Alcoholism, clinical and experimental research · 2011Review
- Tissue-specific N terminus of the HCN4 channel affects channel activation.The Journal of biological chemistry · 2011Article
- A state-dependent salt-bridge interaction exists across the β/α intersubunit interface of the GABAA receptor.Molecular pharmacology · 2011Article
- HSV delivery of a ligand-regulated endogenous ion channel gene to sensory neurons results in pain control following channel activation.Molecular therapy : the journal of the American Society of Gene Therapy · 2011Article
- Pulsed electron spin resonance resolves the coordination site of Cu²(+) ions in α1-glycine receptor.Biophysical journal · 2010Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
Abstract
Proper regulation of neurotransmission requires that ligand-activated ion channels remain closed until agonist binds. How channels then open remains poorly understood. Glycine receptor (GlyR) gating is initiated by agonist binding at interfaces between adjacent subunits in the extracellular domain. Aspartate-97, located at the alpha1 GlyR interface, is a conserved residue in the cys-loop receptor superfamily. The mutation of D97 to arginine (D97R) causes spontaneous channel opening, with open and closed dwell times similar to those of maximally activated WT GlyR. Using a model of the N-terminal domain of the alpha1 GlyR, we hypothesized that an arginine-119 residue was forming intersubunit electrostatic bonds with D97. The D97R/R119E charge reversal restored this interaction, stabilizing channels in their closed states. Cysteine substitution shows that this link occurs between adjacent subunits. This intersubunit electrostatic interaction among GlyR subunits thus contributes to the stabilization of the closed channel state, and its disruption represents a critical step in GlyR activation.
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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.