Inhibiting uptake activity of organic anion transporter 2 by bile acids.
Bile acid
Cholestasis
MDCK-hOAT2
SLC22A7
SNP
Journal
Drug metabolism and pharmacokinetics
ISSN: 1880-0920
Titre abrégé: Drug Metab Pharmacokinet
Pays: England
ID NLM: 101164773
Informations de publication
Date de publication:
Apr 2022
Apr 2022
Historique:
received:
16
07
2021
revised:
17
12
2021
accepted:
18
01
2022
pubmed:
23
2
2022
medline:
17
3
2022
entrez:
22
2
2022
Statut:
ppublish
Résumé
Bile acids, a series of amphiphilic molecules, can interact with several drug transporters and impact drug ADME. Organic anion transporter 2 (OAT2) is exclusively expressed in the liver and kidney. However, the interaction between bile acids and hOAT2 is unelucidated. In this study, we observed that chenodeoxycholic acid, deoxycholic acid, ursodeoxycholic acid, glycochenodeoxycholic acid (GCDCA), glycodeoxycholic acid, glycoursodeoxycholic acid (GUDCA), taurocholic acid (TCA), taurochenodeoxycholic acid (TCDCA), taurodeoxycholic acid, tauroursodeoxycholic acid could all inhibit uptake activity of hOAT2 while glycocholic acid (GCA) and cholic acid could not. Among them, TCDCA was the strongest inhibitor with IC
Identifiants
pubmed: 35190308
pii: S1347-4367(22)00005-2
doi: 10.1016/j.dmpk.2022.100448
pii:
doi:
Substances chimiques
Bile Acids and Salts
0
Membrane Transport Proteins
0
Organic Anion Transporters
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
100448Informations de copyright
Copyright © 2022 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.