Human P-glycoprotein as a multi-drug transporter analyzed by using transepithelial transport system.
To analyze the mechanism of drug transport, mechanism of inhibitors, and physiological substrates of human P-glycoprotein, we established a transepithelial transport system by introducing MDR1 cDNA into LLC-PK1, a pig kidney epithelial cell line. P-glycoprotein functions as a steroid transporter as well as a drug transporter as physiological functions. P-glycoprotein also transports MDR modulators such as cyclosporin A, FK506, and calcium channel blockers.
Ueda
K
K
Department of Agricultural Chemistry, Kyoto University Hospital, Japan.
Saeki
T
T
Hirai
M
M
Tanigawara
Y
Y
Tanaka
K
K
Okamura
M
M
Yasuhara
M
M
Hori
R
R
Inui
K
K
Komano
T
T
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism*; D002352:Carrier Proteins; D016572:Cyclosporine / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D004848:Epithelium; D006801:Humans; D006854:Hydrocortisone / Q000494:pharmacology; D016559:Tacrolimus / Q000494:pharmacology; D014747:Vinblastine / Q000494:pharmacology
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D002352:Carrier Proteins; D014747:Vinblastine; D016572:Cyclosporine; D006854:Hydrocortisone; D016559:Tacrolimus