Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines (Q27674189)

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9 March 2020

title

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines (English)

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9 March 2020

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ChEBI release 2020-05-28

3

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Margot Ernst

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Hugues Nury

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Pierre Legrand

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Werner Sieghart

14

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Sarah C R Lummis

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author name string

Radovan Spurny

1

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Joachim Ramerstorfer

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Marijke Brams

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Mark Verheij

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Daniel Bertrand

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Sonia Bertrand

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Dennis A Dougherty

11

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Iwan J P de Esch

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Chris Ulens

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Pierre-Jean Corringer

13

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language of work or name

English

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publication date

3 October 2012

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Proceedings of the National Academy of Sciences of the United States of America

9 March 2020

published in

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volume

109

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issue

44

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page(s)

E3028-34

1 reference

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Structure of the pentameric ligand-gated ion channel ELIC cocrystallized with its competitive antagonist acetylcholine

9 March 2020

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1 reference

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Crystal Structures of a Cysteine-modified Mutant in Loop D of Acetylcholine-binding Protein

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X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation

20 March 2017

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20 March 2017

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X-ray structure of a prokaryotic pentameric ligand-gated ion channel

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Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors

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A single histidine in GABAA receptors is essential for benzodiazepine agonist binding

20 March 2017

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Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures

20 March 2017

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Two amino acid residues contribute to a cation-π binding interaction in the binding site of an insect GABA receptor

7 April 2017

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Three arginines in the GABAA receptor binding pocket have distinct roles in the formation and stability of agonist- versus antagonist-bound complexes

29 September 2017

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Different Residues in the GABAAReceptor Benzodiazepine Binding Pocket Mediate Benzodiazepine Efficacy and Binding

29 September 2017

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In Search of Allosteric Modulators of α7-nAChR by Solvent Density Guided Virtual Screening

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The GABAA receptor alpha beta- interface: a novel target for subtype selective drugs

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A Closer Look at the High Affinity Benzodiazepine Binding Site on GABAA Receptors

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Covalent modification of GABAA receptor isoforms by a diazepam analogue provides evidence for a novel benzodiazepine binding site that prevents modulation by these drugs

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Unnatural amino acid mutagenesis of the GABA(A) receptor binding site residues reveals a novel cation-pi interaction between GABA and beta 2Tyr97

29 September 2017

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29 September 2017

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29 September 2017

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29 September 2017

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29 September 2017

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Residues at Positions 206 and 209 of the α1 Subunit of γ-Aminobutyric AcidAReceptors Influence Affinities for Benzodiazepine Binding Site Ligands

29 September 2017

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Two tyrosine residues on the alpha subunit are crucial for benzodiazepine binding and allosteric modulation of gamma-aminobutyric acidA receptors

29 September 2017

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29 September 2017

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29 September 2017

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The major site of photoaffinity labeling of the gamma-aminobutyric acid type A receptor by [3H]flunitrazepam is histidine 102 of the alpha subunit.

2 June 2018

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GABAA receptor needs two homologous domains of the beta-subunit for activation by GABA but not by pentobarbital

2 June 2018

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gamma-Aminobutyric acid receptor complex of insect CNS: characterization of a benzodiazepine binding site

2 June 2018

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Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor

2 June 2018

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A cation-pi binding interaction with a tyrosine in the binding site of the GABAC receptor

2 June 2018

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Binding sites for [(3)H]GABA, [(3)H]flunitrazepam and [(35)S]TBPS in insect CNS.

21 January 2018

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Structural determinants for alpha-neurotoxin sensitivity in muscle nAChR and their implications for the gating mechanism

21 January 2018

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A (beta)-strand in the (gamma)2 subunit lines the benzodiazepine binding site of the GABA A receptor: structural rearrangements detected during channel gating.

27 November 2018

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Mutagenesis of the rat alpha1 subunit of the gamma-aminobutyric acid(A) receptor reveals the importance of residue 101 in determining the allosteric effects of benzodiazepine site ligands.

27 November 2018

1 reference

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Mapping the agonist binding site of the GABAA receptor: evidence for a beta-strand.

27 November 2018

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Point mutations of the alpha 1 beta 2 gamma 2 gamma-aminobutyric acid(A) receptor affecting modulation of the channel by ligands of the benzodiazepine binding site.

27 November 2018

1 reference

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Identification of benzodiazepine binding site residues in the gamma2 subunit of the gamma-aminobutyric acid(A) receptor

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/23035248

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1073/PNAS.1208208109

2 references

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23035248 AND SRC:MED&resulttype=core&format=json

9 March 2020

ADS bibcode

2012PNAS..109E3028S

0 references

1 reference

2 references

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23035248 AND SRC:MED&resulttype=core&format=json

9 March 2020

PubMed publication ID

23035248

2 references

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:23035248 AND SRC:MED&resulttype=core&format=json