Agonists and allosteric modulators promote signaling from different metabotropic glutamate receptor 5 conformations.
Cryoelectron Microscopy
Crystallography, X-Ray
Excitatory Amino Acid Agonists
/ metabolism
Excitatory Amino Acid Antagonists
/ metabolism
HEK293 Cells
Humans
Models, Molecular
Protein Binding
Protein Interaction Domains and Motifs
Protein Stability
Protein Subunits
Receptor, Metabotropic Glutamate 5
/ agonists
Signal Transduction
/ drug effects
Structure-Activity Relationship
G-protein-coupled receptors
X-ray crystallography
allosteric modulators
cryo-EM
glutamate
metabotropic glutamate receptor 5
photochromic ligands
signal transduction
Journal
Cell reports
ISSN: 2211-1247
Titre abrégé: Cell Rep
Pays: United States
ID NLM: 101573691
Informations de publication
Date de publication:
31 08 2021
31 08 2021
Historique:
received:
04
03
2021
revised:
08
06
2021
accepted:
11
08
2021
entrez:
1
9
2021
pubmed:
2
9
2021
medline:
15
2
2022
Statut:
ppublish
Résumé
Metabotropic glutamate receptors (mGluRs) are dimeric G-protein-coupled receptors activated by the main excitatory neurotransmitter, L-glutamate. mGluR activation by agonists binding in the venus flytrap domain is regulated by positive (PAM) or negative (NAM) allosteric modulators binding to the 7-transmembrane domain (7TM). We report the cryo-electron microscopy structures of fully inactive and intermediate-active conformations of mGlu
Identifiants
pubmed: 34469715
pii: S2211-1247(21)01091-3
doi: 10.1016/j.celrep.2021.109648
pmc: PMC8424648
pii:
doi:
Substances chimiques
Excitatory Amino Acid Agonists
0
Excitatory Amino Acid Antagonists
0
GRM5 protein, human
0
Protein Subunits
0
Receptor, Metabotropic Glutamate 5
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
109648Subventions
Organisme : Medical Research Council
ID : MC_U105184326
Pays : United Kingdom
Informations de copyright
Copyright © 2021 The Authors. Published by Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of interests The authors declare no competing interests.
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