Crystal structure of human glycine receptor-α3 bound to antagonist strychnine

No abstract is available for this paper.

• Publication year

  2015

• Venue

  Nature

• Publication date

  2015-09-28

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1038/nature14972PMID 26416729
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Allosteric and hyperekplexic mutant phenotypes investigated on an α1 glycine receptor transmembrane structure

  2015cited by this paper
• X-ray structures of GluCl in apo states reveal a gating mechanism of Cys-loop receptors

  2014cited by this paper
• X-ray structure of the mouse serotonin 5-HT3 receptor

  2014cited by this paper
• Crystal structure of a human GABAA receptor

  2014cited by this paper
• Agonist and antagonist binding in human glycine receptors.

  2014cited by this paper
• The impact of human hyperekplexia mutations on glycine receptor structure and function

  2014cited by this paper
• Structure–Activity Relationships of Strychnine Analogs at Glycine Receptors

  2014cited by this paper
• Crystal structures of a pentameric ligand-gated ion channel provide a mechanism for activation

  2013cited by this paper
• A gating mechanism of pentameric ligand-gated ion channels

  2013cited by this paper
• Molecular actions of smoking cessation drugs at α4β2 nicotinic receptors defined in crystal structures of a homologous binding protein

  2012cited by this paper
• A Structural and Mutagenic Blueprint for Molecular Recognition of Strychnine and d-Tubocurarine by Different Cys-Loop Receptors

  2011cited by this paper
• Principles of activation and permeation in an anion-selective Cys-loop receptor

  2011cited by this paper
• Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel

  2009cited by this paper
• X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation

  2009cited by this paper
• X-ray structure of a prokaryotic pentameric ligand-gated ion channel

  2008cited by this paper
• Clustal W and Clustal X version 2.0

  2007cited by this paper
• MolProbity: all-atom contacts and structure validation for proteins and nucleic acids

  2007cited by this paper
• Pharmacological characterisation of strychnine and brucine analogues at glycine and alpha7 nicotinic acetylcholine receptors.

  2006cited by this paper
• Solving structures of protein complexes by molecular replacement with Phaser

  2006cited by this paper
• Glycine receptors: a new therapeutic target in pain pathways.

  2006cited by this paper
• Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations

  2005cited by this paper
• Functional characterisation of the human alpha1 glycine receptor in a fluorescence-based membrane potential assay.

  2004cited by this paper
• Coot: model-building tools for molecular graphics.

  2004cited by this paper
• Molecular structure and function of the glycine receptor chloride channel.

  2004cited by this paper
• Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures.

  2004cited by this paper
• PRODRG: a tool for high-throughput crystallography of protein-ligand complexes.

  2004cited by this paper
• The PyMOL Molecular Graphics System

  2002cited by this paper
• Modulation of glycine receptor function: a novel approach for therapeutic intervention at inhibitory synapses?

  2002cited by this paper
• The glycinergic inhibitory synapse

  2001cited by this paper
• Electrostatics of nanosystems: Application to microtubules and the ribosome

  2001cited by this paper
• Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors

  2001cited by this paper
• The glycine receptor.

  1997cited by this paper
• Refinement of macromolecular structures by the maximum-likelihood method.

  1997cited by this paper
• Processing of X-ray diffraction data collected in oscillation mode.

  1997cited by this paper
• [20] Processing of X-ray diffraction data collected in oscillation mode.

  1997cited by this paper
• HOLE: a program for the analysis of the pore dimensions of ion channel structural models.

  1996cited by this paper
• Antagonism of ligand-gated ion channel receptors: two domains of the glycine receptor alpha subunit form the strychnine-binding site.

  1992cited by this paper
• Alpha subunit variants of the human glycine receptor: primary structures, functional expression and chromosomal localization of the corresponding genes.

  1990cited by this paper
• Conserved quaternary structure of ligand-gated ion channels: the postsynaptic glycine receptor is a pentamer.

  1988cited by this paper
• Glycine receptor heterogeneity in rat spinal cord during postnatal development.

  1988cited by this paper
• Sequence and functional expression of the GABAA receptor shows a ligand-gated receptor super-family

  1987cited by this paper

• Computation suggests that the cell adhesion sub-proteome is enriched for sites of pH-dependence and charge burial

  2025cites this paper
• Allosteric modulation and direct activation of glycine receptors by a tricyclic sulfonamide

  2025cites this paper
• The function of chloride channels in digestive system disease (Review)

  2025cites this paper
• State-Dependent Dynamic Communication Networks in a Pentameric Ligand-Gated Ion Channel.

  2025cites this paper
• Deciphering the molecular mechanisms of startle disease: The role of the Asn46Lys mutation in the glycine receptor.

  2025cites this paper
• Mechanism of human α3β GlyR regulation by intracellular M3/M4 loop phosphorylation and 2,6-di-tert-butylphenol interaction

  2025cites this paper
• In Silico Characterization of Gelsemium Compounds as Glycine Receptor Ligands

  2025cites this paper
• Structural insights into the activation mechanism of the human zinc-activated channel

  2025cites this paper
• The emerging role of glycine receptor α2 subunit defects in neurodevelopmental disorders

  2025cites this paper
• Glycine receptors: Structure, function, and therapeutic implications.

  2025cites this paper
• 三聚体配体门控离子通道胞内区域的功能研究进展

  2024cites this paper
• Structural Basis for Molecular Recognition of Cannabinoids by Inhibitory Cys-Loop Channels.

  2024cites this paper
• Structural insights into the molecular effects of the anthelmintics monepantel and betaine on the Caenorhabditis elegans acetylcholine receptor ACR-23

  2024cites this paper
• Exploring the Activation Process of the Glycine Receptor.

  2024cites this paper
• Gating mechanism of the human α1β GlyR by glycine.

  2024cites this paper
• Cryo-EM structure of the zinc-activated channel (ZAC) in the Cys-loop receptor superfamily

  2024cites this paper
• Modulation of heteromeric glycine receptor function through high concentration clustering

  2024cites this paper
• Electrically silent mutants unravel the mechanism of binding-gating coupling in Cys-loop receptors.

  2024cites this paper
• Mechanisms underlying modulation of human GlyRα3 by Zn2+ and pH

  2024cites this paper
• Molecular Pharmacology of Gelsemium Alkaloids on Inhibitory Receptors

  2024cites this paper
• The mRNA expression profile of glycine receptor subunits alpha 1, alpha 2, alpha 4 and beta in female and male mice.

  2024cites this paper
• Conformational transitions and allosteric modulation in a heteromeric glycine receptor

  2023cites this paper
• Alkaline taste sensation through the alkaliphile chloride channel in Drosophila

  2023cites this paper
• Asymmetric gating of a human hetero-pentameric glycine receptor

  2023cites this paper
• Asymmetric gating of a human hetero-pentameric glycine receptor

  2023cites this paper
• Convergent and divergent evolution of plant chemical defenses.

  2023cites this paper
• AAV-glycine receptor α3 alleviates CFA-induced inflammatory pain by downregulating ERK phosphorylation and proinflammatory cytokine expression in SD rats

  2023cites this paper
• Repurposing of Anti-Infectives for the Management of Onchocerciasis Using Machine Learning and Protein Docking Studies

  2023cites this paper
• Gating mechanism of the human α1β GlyR by glycine

  2023cites this paper
• Role of the Glycine Receptor β Subunit in Synaptic Localization and Pathogenicity in Severe Startle Disease

  2023cites this paper
• Modelling and Molecular Dynamics Predict the Structure and Interactions of the Glycine Receptor Intracellular Domain

  2023cites this paper
• Glycine receptor autoantibody binding to the extracellular domain is independent from receptor glycosylation

  2023influential citation
• Methodological Development and Applications of Tryptamine-Ynamide Cyclizations in Synthesizing Core Skeletons of Indole Alkaloids.

  2023cites this paper
• Structural Biology-Guided Design, Synthesis, and Biological Evaluation of Novel Insect Nicotinic Acetylcholine Receptor Orthosteric Modulators.

  2022cites this paper
• GLRA2 gene mutations cause high myopia in humans and mice

  2022cites this paper
• Loss, Gain and Altered Function of GlyR α2 Subunit Mutations in Neurodevelopmental Disorders

  2022cites this paper
• Expression of Mutant Glycine Receptors in Xenopus Oocytes Using Canonical and Non-Canonical Amino Acids Reveals Distinct Roles of Conserved Proline Residues

  2022cites this paper
• Molecular determinants of tetrahydrocannabinol binding to the glycine receptor

  2022cites this paper
• Neurotransmitter systems in zebrafish model as a target for neurobehavioural studies

  2022cites this paper
• Modulation of Ligand-Gated Glycine Receptors Via Functional Monoclonal Antibodies

  2022influential citation
• Exploring the Conformational Impact of Glycine Receptor TM1-2 Mutations Through Coarse-Grained Analysis and Atomistic Simulations

  2022cites this paper
• Structure and Mechanism of Glycine Receptor Elucidated by Cryo-Electron Microscopy

  2022influential citation
• Structural basis for cannabinoid-induced potentiation of alpha1-glycine receptors in lipid nanodiscs

  2022cites this paper
• Pentameric assembly of glycine receptor intracellular domains provides insights into gephyrin clustering

  2022cites this paper
• Mutations of the nACh Receptor M4 Helix Reveal Different Phenotypes in Different Expression Systems: Could Lipids be Responsible?

  2022cites this paper
• Lateral fenestrations in the extracellular domain of the glycine receptor contribute to the main chloride permeation pathway

  2022cites this paper
• Biosynthesis of strychnine

  2022cites this paper
• Insect RDL Receptor Models for Virtual Screening: Impact of the Template Conformational State in Pentameric Ligand-Gated Ion Channels

  2022cites this paper
• The glycine-containing dipeptide leucine-glycine raises accumbal dopamine levels in a subpopulation of rats presenting a lower endogenous dopamine tone

  2022cites this paper
• Startle Disease: New Molecular Insights into an Old Neurological Disorder

  2022cites this paper
• Structural basis for strychnine activation of human bitter taste receptor TAS2R46

  2022cites this paper
• Glycine Receptor Subtypes and Their Roles in Nociception and Chronic Pain

  2022cites this paper
• The structural patterns of the potentiation and the blockade of inhibitory cys-loop receptors through the transmembrane domain

  2022cites this paper
• Computational Investigation of Mechanisms for pH Modulation of Human Chloride Channels

  2022cites this paper
• Strychnine and its mono- and dimeric analogues: a pharmaco-chemical perspective.

  2022cites this paper
• Regulation of a pentameric ligand-gated ion channel by a semiconserved cationic lipid-binding site

  2021cites this paper
• An Inside Job: Molecular Determinants for Postsynaptic Localization of Nicotinic Acetylcholine Receptors

  2021cites this paper
• A Single Mutation in the Outer Lipid-Facing Helix of a Pentameric Ligand-Gated Ion Channel Affects Channel Function Through a Radially-Propagating Mechanism

  2021cites this paper
• Recombinant expression and purification of pentameric ligand-gated ion channels for Cryo-EM structural studies.

  2021cites this paper
• Glycine Receptors in Spinal Nociceptive Control—An Update

  2021cites this paper
• A cationic lipid site at the outward transmembrane face of a pentameric ligand-gated ion channel

  2021cites this paper
• Signal transduction through Cys-loop receptors is mediated by the nonspecific bumping of closely apposed domains

  2021cites this paper
• Highlighting membrane protein structure and function: A celebration of the Protein Data Bank

  2021cites this paper
• The intracellular domain of homomeric glycine receptors modulates agonist efficacy

  2021cites this paper
• Glycine is a competitive antagonist of the TNF receptor mediating the expression of inflammatory cytokines in 3T3-L1 adipocytes

  2021cites this paper
• C-2-Linked Dimeric Strychnine Analogues as Bivalent Ligands Targeting Glycine Receptors.

  2021cites this paper
• Computational Ion Channel Research: from the Application of Artificial Intelligence to Molecular Dynamics Simulations.

  2021cites this paper
• Elephants in the dark: insights and incongruities in pentameric ligand-gated ion channel models.

  2021cites this paper
• Identification and pharmacological characterization of histamine-gated chloride channels in the fall armyworm, Spodoptera frugiperda.

  2021cites this paper
• Different Behaviors of a Glycine Receptor Channel Pore Residue between Wild-Type-Mimicking and Disease-Type-Mimicking Formats.

  2021cites this paper
• Novel Functional Properties of Missense Mutations in the Glycine Receptor β Subunit in Startle Disease

  2021cites this paper
• Glycine receptors in GtoPdb v.2021.3

  2021cites this paper
• Characterization of the subunit composition and structure of adult human glycine receptors.

  2021cites this paper
• Mechanism of gating and partial agonist action in the glycine receptor.

  2021cites this paper
• Progress in nicotinic receptor structural biology.

  2020cites this paper
• Structure of the Native Muscle-type Nicotinic Receptor and Inhibition by Snake Venom Toxins.

  2020cites this paper
• State-dependent protein-lipid interactions of a pentameric ligand-gated ion channel in a neuronal membrane

  2020cites this paper
• The MX-Helix of Muscle nAChR Subunits Regulates Receptor Assembly and Surface Trafficking

  2020cites this paper
• Role of Glycine Receptor α3 in the Phosphorylation of Extracellular Signal-Regulated Kinase by Prostaglandin E2

  2020cites this paper
• Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site

  2020influential citation
• Comparing Cryo-EM Reconstructions and Validating Atomic Model Fit Using Difference Maps

  2020cites this paper
• Structural basis for the modulation of pentameric ligand-gated ion channel function by lipids.

  2020cites this paper
• The intracellular domain of homomeric glycine receptors modulates agonist efficacy.

  2020cites this paper
• Thermophoretic analysis of ligand-specific conformational states of the inhibitory glycine receptor embedded in copolymer nanodiscs

  2020cites this paper
• Fine-Tuning of Neuronal Ion Channels-Mapping of Residues Involved in Glucose Sensitivity of Recombinant Human Glycine Receptors.

  2020cites this paper
• Change the channel: CysLoop receptor antagonists from Nature.

  2020cites this paper
• Important amino acids for function of the insect Rdl GABA receptor.

  2020cites this paper
• Fluorescence-detection size-exclusion chromatography utilizing nanobody technology for expression screening of membrane proteins

  2020cites this paper
• Proline Residues Contribute to Efficient GABAp Receptor Function.

  2020cites this paper
• Strychnine

  2020cites this paper
• Charged residues at the pore extracellular half of the glycine receptor facilitate channel gating: a potential role played by electrostatic repulsion

  2020cites this paper
• Thermodynamics and Kinetics of Ion Permeation in Wild-Type and Mutated Open Active Conformation of the Human α7 Nicotinic Receptor

  2020cites this paper
• Sequential purification and characterization of Torpedo californica nAChR-DC supplemented with CHS for high-resolution crystallization studies.

  2020cites this paper
• A pair of residue substitutions at the outer mouth of the channel pore act as inputs for a Boolean logic "OR" gate based on the glycine receptor.

  2020cites this paper
• Ligand-gated ion channels in genetic disorders and the question of efficacy.

  2020cites this paper
• Mechanisms of activation and desensitization of full-length glycine receptor in lipid nanodiscs

  2020cites this paper
• Many Proline Residues in the Extracellular Domain Contribute to Glycine Receptor Function.

  2020cites this paper
• Structural basis for allosteric transitions of a multidomain pentameric ligand-gated ion channel

  2020cites this paper
• Modulators of the inhibitory glycine receptor.

  2020cites this paper
• GlyR autoantibodies impair receptor function and induce motor dysfunction.

  2020cites this paper