Probing the correlation between ligand efficacy and conformational diversity at the α
G protein-coupled receptor (GPCR)
adrenergic receptor
allosteric coupling
binding mechanism
conformational change
conformational equilibrium
ligand-binding protein
microswitch
nuclear magnetic resonance (NMR)
solution structure
Journal
The Journal of biological chemistry
ISSN: 1083-351X
Titre abrégé: J Biol Chem
Pays: United States
ID NLM: 2985121R
Informations de publication
Date de publication:
22 05 2020
22 05 2020
Historique:
received:
31
01
2020
revised:
14
04
2020
pubmed:
19
4
2020
medline:
29
12
2020
entrez:
19
4
2020
Statut:
ppublish
Résumé
G protein-coupled receptors (GPCRs) use a series of conserved microswitches to transmit signals across the cell membrane via an allosteric network encompassing the ligand-binding site and the G protein-binding site. Crystal structures of GPCRs provide snapshots of their inactive and active states, but poorly describe the conformational dynamics of the allosteric network that underlies GPCR activation. Here, we analyzed the correlation between ligand binding and receptor conformation of the α
Identifiants
pubmed: 32303636
pii: S0021-9258(17)50272-0
doi: 10.1074/jbc.RA120.012842
pmc: PMC7247315
pii:
doi:
Substances chimiques
ADRA1A protein, human
0
Ligands
0
Receptors, Adrenergic, alpha-1
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
7404-7417Informations de copyright
© 2020 Wu et al.
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