Inhibition of organic cation transporter (OCT) activities by carcinogenic heterocyclic aromatic amines.
Drug transporter
Heterocyclic amines
Organic cation transporter
Toxicity
Toxicokinetics
Journal
Toxicology in vitro : an international journal published in association with BIBRA
ISSN: 1879-3177
Titre abrégé: Toxicol In Vitro
Pays: England
ID NLM: 8712158
Informations de publication
Date de publication:
Feb 2019
Feb 2019
Historique:
received:
18
05
2018
revised:
30
08
2018
accepted:
31
08
2018
pubmed:
7
9
2018
medline:
15
1
2019
entrez:
7
9
2018
Statut:
ppublish
Résumé
Carcinogenic heterocyclic aromatic amines (HAAs) interact with some drug transporters, like the efflux pump BCRP and the organic anion transporters OAT1 and OAT3. The present study was designed to determine whether they can also target activities of the organic cation transporters (OCTs), using mainly OCT1-, OCT2- and OCT3-overexpressing HEK293 cells. Fifteen HAAs were demonstrated to differently alter OCT activities; with a cut-off of at least 50% reduction of transporter activity by 100 μM HAAs, 5/15 HAAs, including Trp-P-1 and Trp-P-2, inhibited activities of OCT1, OCT2 and OCT3, whereas 7/15 HAAs, including PhIP and MeIQx, blocked those of OCT2 and OCT3, 1/15 HAAs reduced those of OCT1 and OCT2 and 2/15 HAAs, including AαC, only that of OCT2. IC
Identifiants
pubmed: 30189235
pii: S0887-2333(18)30190-5
doi: 10.1016/j.tiv.2018.08.015
pii:
doi:
Substances chimiques
Amines
0
Heterocyclic Compounds
0
Organic Cation Transport Proteins
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
10-22Informations de copyright
Copyright © 2018 Elsevier Ltd. All rights reserved.