Differences in transport function of the human and rat orthologue of the Organic Anion Transporting Polypeptide 2B1 (OATP2B1).
Estrone 3-sulfate
OATP2B1
Species-differences
Substrate recognition
Journal
Drug metabolism and pharmacokinetics
ISSN: 1880-0920
Titre abrégé: Drug Metab Pharmacokinet
Pays: England
ID NLM: 101164773
Informations de publication
Date de publication:
Dec 2021
Dec 2021
Historique:
received:
07
04
2021
revised:
30
06
2021
accepted:
17
08
2021
pubmed:
11
10
2021
medline:
14
1
2022
entrez:
10
10
2021
Statut:
ppublish
Résumé
The human drug transporter Organic Anion Transporting Polypeptide (hOATP)2B1 facilitates cellular uptake of its substrates. Various studies suggest that hOATP2B1 is involved in intestinal absorption, but preclinical evaluations performed in rodents do not support this. Thus, our study aimed to compare the expression and function of hOATP2B1 with its orthologue in rats (rOatp2b1). Even if the general expression pattern was comparable, the transporters exhibited substantial differences on functional level. While bromosulfophthalein and atorvastatin were substrates of both transporters, the steroid sulfate conjugates estrone 3-sulfate (E
Identifiants
pubmed: 34628357
pii: S1347-4367(21)00039-2
doi: 10.1016/j.dmpk.2021.100418
pii:
doi:
Substances chimiques
Organic Anion Transporters
0
oatp2b1 protein, rat
0
Estrone
2DI9HA706A
Atorvastatin
A0JWA85V8F
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
100418Informations de copyright
Copyright © 2021 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest None of the authors have a conflict of interest to declare.