Allosteric ligands control the activation of a class C GPCR heterodimer by acting at the transmembrane interface.
G protein
GABA-B
allosteric agonism
allosteric modulator
biochemistry
chemical biology
human
metabotropic glutamate receptor
oligomer
Journal
eLife
ISSN: 2050-084X
Titre abrégé: Elife
Pays: England
ID NLM: 101579614
Informations de publication
Date de publication:
06 12 2021
06 12 2021
Historique:
received:
09
05
2021
accepted:
02
12
2021
pubmed:
7
12
2021
medline:
27
1
2022
entrez:
6
12
2021
Statut:
epublish
Résumé
G protein-coupled receptors (GPCRs) are among the most promising drug targets. They often form homo- and heterodimers with allosteric cross-talk between receptor entities, which contributes to fine-tuning of transmembrane signaling. Specifically controlling the activity of GPCR dimers with ligands is a good approach to clarify their physiological roles and validate them as drug targets. Here, we examined the mode of action of positive allosteric modulators (PAMs) that bind at the interface of the transmembrane domains of the heterodimeric GABA
Identifiants
pubmed: 34866572
doi: 10.7554/eLife.70188
pii: 70188
pmc: PMC8700296
doi:
pii:
Substances chimiques
Ligands
0
Receptors, GABA-B
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Informations de copyright
© 2021, Liu et al.
Déclaration de conflit d'intérêts
LL, ZF, XR, LX, SR, IB, MX, JP, PR, JL No competing interests declared
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