Natural biased signaling of hydroxycarboxylic acid receptor 3 and G protein-coupled receptor 84.
Dynamin-2
GPCR
GPR109b
GPR84
HCA3
HCAR
Hydroxycarboxylic acid receptors
Journal
Cell communication and signaling : CCS
ISSN: 1478-811X
Titre abrégé: Cell Commun Signal
Pays: England
ID NLM: 101170464
Informations de publication
Date de publication:
26 02 2020
26 02 2020
Historique:
received:
15
10
2019
accepted:
29
01
2020
entrez:
28
2
2020
pubmed:
28
2
2020
medline:
9
7
2021
Statut:
epublish
Résumé
Medium-chain fatty acids and their 3-hydroxy derivatives are metabolites endogenously produced in humans, food-derived or originating from bacteria. They activate G protein-coupled receptors, including GPR84 and HCA To study the signaling kinetics and components involved in signal transduction of both receptors we applied the label-free dynamic mass redistribution technology in combination with classical cAMP, ERK signaling and β-arrestin-2 recruitment assays. For phenotypical analyses, we used spheroid cell culture models. We present strong evidence for a natural biased signaling of structurally highly similar agonists at HCA In summary, our results highlight that biased agonism is a physiological property of HCA
Sections du résumé
BACKGROUND
Medium-chain fatty acids and their 3-hydroxy derivatives are metabolites endogenously produced in humans, food-derived or originating from bacteria. They activate G protein-coupled receptors, including GPR84 and HCA
METHODS
To study the signaling kinetics and components involved in signal transduction of both receptors we applied the label-free dynamic mass redistribution technology in combination with classical cAMP, ERK signaling and β-arrestin-2 recruitment assays. For phenotypical analyses, we used spheroid cell culture models.
RESULTS
We present strong evidence for a natural biased signaling of structurally highly similar agonists at HCA
CONCLUSIONS
In summary, our results highlight that biased agonism is a physiological property of HCA
Identifiants
pubmed: 32102673
doi: 10.1186/s12964-020-0516-2
pii: 10.1186/s12964-020-0516-2
pmc: PMC7045412
doi:
Substances chimiques
GPR84 protein, human
0
HCAR3 protein, human
0
Receptors, G-Protein-Coupled
0
Receptors, Nicotinic
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Video-Audio Media
Langues
eng
Sous-ensembles de citation
IM
Pagination
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