Interaction modes of human orexin 2 receptor with selective and nonselective antagonists studied by NMR spectroscopy.
(13)C methyl methionine NMR
EMPA
GPCR
OX2R
orexin 2 receptor
structural plasticity
suvorexant
Journal
Structure (London, England : 1993)
ISSN: 1878-4186
Titre abrégé: Structure
Pays: United States
ID NLM: 101087697
Informations de publication
Date de publication:
01 Jan 2024
01 Jan 2024
Historique:
received:
24
02
2023
revised:
17
08
2023
accepted:
13
12
2023
medline:
10
1
2024
pubmed:
10
1
2024
entrez:
9
1
2024
Statut:
aheadofprint
Résumé
Orexin neuropeptides have many physiological roles in the sleep-wake cycle, feeding behavior, reward demands, and stress responses by activating cognitive receptors, the orexin receptors (OX1R and OX2R), distributed in the brain. There are only subtle differences between OX1R and OX2R in the orthosteric site, which has hindered the rational development of subtype-selective antagonists. In this study, we utilized solution-state NMR to capture the structural plasticity of OX2R labeled with
Identifiants
pubmed: 38194963
pii: S0969-2126(23)00449-5
doi: 10.1016/j.str.2023.12.008
pii:
doi:
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Informations de copyright
Copyright © 2023 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of interests The authors declare no conflict of interest.