Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation.
BHB
GPCR
HCAR2
allosteric modulation
anti-inflamation
biased allosteric modulator
cryo-EM
ketone body receptor
niacin
structural biology
Journal
Molecular cell
ISSN: 1097-4164
Titre abrégé: Mol Cell
Pays: United States
ID NLM: 9802571
Informations de publication
Date de publication:
07 09 2023
07 09 2023
Historique:
received:
22
02
2023
revised:
27
06
2023
accepted:
28
07
2023
medline:
11
9
2023
pubmed:
20
8
2023
entrez:
19
8
2023
Statut:
ppublish
Résumé
Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone body β-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for inflammation-related diseases. HCAR2 mediates distinct pathophysiological events by activating G
Identifiants
pubmed: 37597514
pii: S1097-2765(23)00605-6
doi: 10.1016/j.molcel.2023.07.030
pii:
doi:
Substances chimiques
GTP-Binding Protein alpha Subunits, Gi-Go
EC 3.6.5.1
Ketone Bodies
0
Niacin
2679MF687A
Hcar2 protein, mouse
0
Receptors, G-Protein-Coupled
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
3171-3187.e7Informations de copyright
Copyright © 2023 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of interests West China Hospital of Sichuan University has applied for a Chinese patent (accepting institution: State Intellectual Property Office [SIPO] in China, patent application number: 2023102433637) on the combination of compound 9n and niacin for the treatment of inflammation-related diseases.