GABA receptor signalling mechanisms revealed by structural pharmacology

scientific article published on 02 January 2019

GABA receptor signalling mechanisms revealed by structural pharmacology is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1038/S41586-018-0832-5
P932PMC publication ID6370056
P698PubMed publication ID30602790

P50authorJan SteyaertQ28050902
Tomas MalinauskasQ28606948
Abhay KotechaQ56437387
Itziar Serna MartinQ57643797
Tomasz UchańskiQ63433859
P2093author name stringA Radu Aricescu
Els Pardon
Keith W Miller
Rooma Desai
Duncan Laverty
Dimple Karia
Jasenko Zivanov
Simonas Masiulis
P2860cites workMolProbity: all-atom structure validation for macromolecular crystallographyQ24649111
Structure, function, and modulation of GABA(A) receptorsQ26859328
Structure and gating mechanism of the acetylcholine receptor poreQ27641514
Crystal structure of a human GABAA receptorQ27644591
Principles of activation and permeation in an anion-selective Cys-loop receptorQ27667848
Helicobacter pylori adhesin HopQ engages in a virulence-enhancing interaction with human CEACAMsQ27728476
Inference of macromolecular assemblies from crystalline stateQ27860457
UCSF Chimera--a visualization system for exploratory research and analysisQ27860666
Features and development of CootQ27861079
The FLAG peptide, a versatile fusion tag for the purification of recombinant proteinsQ28203819
International Union of Pharmacology. XV. Subtypes of gamma-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor functionQ28275171
Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2Q28296477
Bicuculline and gabazine are allosteric inhibitors of channel opening of the GABAA receptorQ28300800
A single histidine in GABAA receptors is essential for benzodiazepine agonist bindingQ28572645
HOLE: a program for the analysis of the pore dimensions of ion channel structural modelsQ29619250
cryoSPARC: algorithms for rapid unsupervised cryo-EM structure determinationQ30398255
Beyond classical benzodiazepines: novel therapeutic potential of GABAA receptor subtypesQ30466591
Hooked on benzodiazepines: GABAA receptor subtypes and addictionQ33607409
Interaction of picrotoxin with GABAA receptor channel-lining residues probed in cysteine mutants.Q34047528
Nicotinic acetylcholine receptor and the structural basis of neuromuscular transmission: insights from Torpedo postsynaptic membranesQ34372276
Structural model for gamma-aminobutyric acid receptor noncompetitive antagonist binding: widely diverse structures fit the same siteQ34597062
A general protocol for the generation of Nanobodies for structural biologyQ34979957
Chapter 11 - Reconstitution of membrane proteins in phospholipid bilayer nanodiscsQ35012211
Anesthetic sites and allosteric mechanisms of action on Cys-loop ligand-gated ion channelsQ35024917
The location of a closed channel gate in the GABAA receptor channel.Q36299672
GABAA receptors in central nervous system disease: anxiety, epilepsy, and insomniaQ36659853
Competitive antagonists facilitate the recovery from desensitization of α1β2γ2 GABAA receptors expressed in Xenopus oocytesQ37151606
Human α1β3γ2L gamma-aminobutyric acid type A receptors: High-level production and purification in a functional stateQ37588964
Advantages of an antagonist: bicuculline and other GABA antagonistsQ38083098
Phosphorylation mediated structural and functional changes in pentameric ligand-gated ion channels: implications for drug discoveryQ38216292
Structure and pharmacology of gamma-aminobutyric acidA receptor subtypes.Q40417870
Desensitization mechanism of GABA receptors revealed by single oocyte binding and receptor function.Q40704823
A lysine residue in the beta3 subunit contributes to the regulation of GABA(A) receptor activity by voltageQ40706305
MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopyQ41598828
Gctf: Real-time CTF determination and correctionQ41603517
Studies on the mechanisms of action of picrotoxin, quercetin and pregnanolone at the GABA rho 1 receptorQ42180848
Mechanisms for picrotoxin block of alpha2 homomeric glycine receptors.Q42675493
Characterization of the picrotoxin site of GABAA receptorsQ42721820
Site-specific fluorescence reveals distinct structural changes with GABA receptor activation and antagonismQ44170924
Individual properties of the two functional agonist sites in GABA(A) receptors.Q44681120
Picrotoxin accelerates relaxation of GABAC receptorsQ45127940
Benzodiazepine receptors in rat brainQ45205253
Allosteric ligands and their binding sites define γ-aminobutyric acid (GABA) type A receptor subtypesQ46744735
Crystal structures of a GABAA-receptor chimera reveal new endogenous neurosteroid-binding sites.Q47246914
Structural basis for GABAA receptor potentiation by neurosteroids.Q47678129
Sequence and functional expression of the GABA A receptor shows a ligand-gated receptor super-familyQ48341437
Analysis of γ-aminobutyric acid (GABA) type A receptor subtypes using isosteric and allosteric ligandsQ48663996
Relative positioning of classical benzodiazepines to the γ2-subunit of GABAA receptorsQ48720997
Isolation of a GABA receptor from bovine brain using a benzodiazepine affinity columnQ48886991
A hydrophobic photolabel inhibits nicotinic acetylcholine receptors via open-channel block following a slow stepQ48906611
A functional comparison of the antagonists bicuculline and picrotoxin at recombinant GABAA receptorsQ49023322
Point mutations in the M2 region of the alpha, beta, or gamma subunit of the GABAA channel that abolish block by picrotoxinQ49071081
GABAA receptor: Positive and negative allosteric modulatorsQ50178492
MonoRes: Automatic and Accurate Estimation of Local Resolution for Electron Microscopy MapsQ50207898
Benzodiazepines act on GABAA receptors via two distinct and separable mechanisms.Q50720910
Real-space refinement in PHENIX for cryo-EM and crystallographyQ54691589
Cryo-EM structure of the benzodiazepine-sensitive α1β1γ2S tri-heteromeric GABA receptor in complex with GABAQ56531762
Structure of a human synaptic GABAA receptorQ56603639
Cryo-EM in drug discovery: achievements, limitations and prospectsQ57178721
New tools for automated high-resolution cryo-EM structure determination in RELION-3Q58563641
New tools for the analysis and validation of cryo-EM maps and atomic modelsQ58767119
Structural basis of neurosteroid anesthetic action on GABA receptorsQ59126131
A Bayesian approach to beam-induced motion correction in cryo-EM single-particle analysisQ61809629
Cryo-EM structure of the human α1β3γ2 GABA receptor in a lipid bilayerQ63432840
Monoclonal antibodies to rhodopsin: characterization, cross-reactivity, and application as structural probesQ72694659
The dual-gate model for pentameric ligand-gated ion channels activation and desensitizationQ87892073
Cryo-EM structure of the human α5β3 GABAA receptorQ91114563
P2507corrigendum / erratumAuthor Correction: GABAA receptor signalling mechanisms revealed by structural pharmacologyQ63432844
P433issue7740
P407language of work or nameEnglishQ1860
P921main subjectpharmacologyQ128406
P304page(s)454-459
P577publication date2019-01-02
P1433published inNatureQ180445
P1476titleGABAA receptor signalling mechanisms revealed by structural pharmacology
P478volume565

Reverse relations

cites work (P2860)
Q90285849A half century of γ-aminobutyric acid
Q90576275A lipid site shapes the agonist response of a pentameric ligand-gated ion channel
Q92438088A minireview of hydroamination catalysis: alkene and alkyne substrate selective, metal complex design
Q89664922A novel de novo variant of GABRA1 causes increased sensitivity for GABA in vitro
Q93072946A photoswitchable GABA receptor channel blocker
Q89895985Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility
Q91148606An in-depth structural view of a GABAA brain receptor
Q89668348Awareness during emergence from anesthesia: Features and future research directions
Q91641482Brexanolone, a neurosteroid antidepressant, vindicates the GABAergic deficit hypothesis of depression and may foster resilience
Q99200516Cryo-EM as a powerful tool for drug discovery
Q63432840Cryo-EM structure of the human α1β3γ2 GABA receptor in a lipid bilayer
Q90428686Cryo-electron microscopy reveals informative details of GABAA receptor structural pharmacology: implications for drug discovery
Q64084725Diazepam Accelerates GABAR Synaptic Exchange and Alters Intracellular Trafficking
Q91961960Effects of Diazepam on Low-Frequency and High-Frequency Electrocortical γ-Power Mediated by α1- and α2-GABAA Receptors
Q93133373Electrophysiological evaluation of extracellular spermine and alkaline pH on synaptic human GABAA receptors
Q92703986GABAA Receptor Ligands Often Interact with Binding Sites in the Transmembrane Domain and in the Extracellular Domain-Can the Promiscuity Code Be Cracked?
Q91312585GABAA receptor structures solved
Q89619699Lack of Neurosteroid Selectivity at δ vs. γ2-Containing GABAA Receptors in Dentate Granule Neurons
Q97904899Mechanisms of activation and desensitization of full-length glycine receptor in lipid nanodiscs
Q92991557Modulation of the Erwinia ligand-gated ion channel (ELIC) and the 5-HT3 receptor via a common vestibule site
Q92034587Molecular mechanism of setron-mediated inhibition of full-length 5-HT3A receptor
Q92510283Neurobiology and Therapeutic Potential of α5-GABA Type A Receptors
Q90376795Phenotypic variability of GABRA1-related epilepsy in monozygotic twins
Q90424652Photopotentiation of the GABAA receptor with caged diazepam
Q93018038Psychotropic Drugs for the Management of Chronic Pain and Itch
Q64078790Robustness of signal detection in cryo-electron microscopy via a bi-objective-function approach
Q89530744Scopoletin ameliorates anxiety-like behaviors in complete Freund's adjuvant-induced mouse model
Q98906941Shared structural mechanisms of general anaesthetics and benzodiazepines
Q99587934Site-specific effects of neurosteroids on GABAA receptor activation and desensitization
Q94654007Spontaneous and evoked neurotransmission are partially segregated at inhibitory synapses
Q92799413Structure of Heteropentameric GABAA Receptors and Receptor-Anchoring Properties of Gephyrin
Q91781302Targeting GABAAR-Associated Proteins: New Modulators, Labels and Concepts
Q90259999The Glycine Receptor Allosteric Ligands Library (GRALL)
Q100958563The desensitization pathway of GABAA receptors, one subunit at a time
Q89523701The effects of a competitive antagonist on GABA-evoked currents in the presence of sedative-hypnotic agents
Q92601431Triple arginines as molecular determinants for pentameric assembly of the intracellular domain of 5-HT3A receptors

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