Effects of MDR1 1236C > T-2677G > T-3435C > T polymorphisms on the intracellular accumulation of tacrolimus, cyclosporine A, sirolimus and everolimus.
ATP Binding Cassette Transporter, Subfamily B
/ genetics
ATP Binding Cassette Transporter, Subfamily B, Member 1
/ metabolism
Animals
Cyclosporine
/ pharmacokinetics
Drug Resistance
Everolimus
/ pharmacokinetics
Humans
Immunosuppressive Agents
/ pharmacokinetics
LLC-PK1 Cells
Polymorphism, Single Nucleotide
Recombinant Proteins
/ genetics
Rhodamine 123
/ pharmacokinetics
Sirolimus
/ pharmacokinetics
Swine
Tacrolimus
/ pharmacokinetics
MDR1 polymorphisms
accumulation
efflux
immunosuppressor
resistance
Journal
Xenobiotica; the fate of foreign compounds in biological systems
ISSN: 1366-5928
Titre abrégé: Xenobiotica
Pays: England
ID NLM: 1306665
Informations de publication
Date de publication:
Nov 2019
Nov 2019
Historique:
pubmed:
28
12
2018
medline:
6
2
2020
entrez:
28
12
2018
Statut:
ppublish
Résumé
1. Overexpression of P-glycoprotein (P-gp, encoded by MDR1) mediates resistance to multiple immunosuppressors. Several common MDR1 variants (1236C > T, 2677G > T, 3435C > T) impact the efflux activity of P-gp-mediated substrates. We assessed the effect of these polymorphisms on the sensitivity, intracellular accumulation, and efflux of tacrolimus, cyclosporine A, sirolimus and everolimus in transfected LLC-PK1 cells. 2. LLC-PK1 cell lines were transfected with empty vector (pcDNA3.1) and recombinant MDR1
Identifiants
pubmed: 30587068
doi: 10.1080/00498254.2018.1563732
doi:
Substances chimiques
ABCB1 protein, human
0
ATP Binding Cassette Transporter, Subfamily B
0
ATP Binding Cassette Transporter, Subfamily B, Member 1
0
Immunosuppressive Agents
0
Recombinant Proteins
0
Rhodamine 123
1N3CZ14C5O
Cyclosporine
83HN0GTJ6D
Everolimus
9HW64Q8G6G
Sirolimus
W36ZG6FT64
Tacrolimus
WM0HAQ4WNM
Types de publication
Journal Article
Video-Audio Media
Langues
eng
Sous-ensembles de citation
IM