Drug transporters: gatekeepers controlling access of xenobiotics to the cellular interior.
In this paper, we evaluate methodologies and null mouse models used to study drug transporter function in vitro and in vivo. P-glycoprotein and MRP null mice have been used to examine many aspects of xenobiotic distribution and bioavailability. Their advantage over conventional models is that they allow the exclusion of transporters from a particular process; however, they cannot be used to study the activity of the transporter that has been deleted. Use of humanized mice permits a logical progression from phenomena in wild-type mice via the effects of removing the mouse transporter to the consequences of replacing it with its human counterpart.
Stanley
Lesley A
LA
lesleystanley@btinternet.com
Horsburgh
Brian C
BC
Ross
Jillian
J
Scheer
Nico
N
Wolf
C Roland
CR
D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D001682:Biological Availability; D001692:Biological Transport / Q000502:physiology*; D001812:Blood-Brain Barrier / Q000378:metabolism; D002451:Cell Compartmentation; D002478:Cells, Cultured; D006801:Humans; D008099:Liver / Q000378:metabolism; D008566:Membranes / Q000378:metabolism; D023421:Models, Animal; D008954:Models, Biological; D010600:Pharmacology / Q000379:methods*; D014018:Tissue Distribution; D015262:Xenobiotics / Q000493:pharmacokinetics* / Q000633:toxicity
D018528:ATP-Binding Cassette Transporters; D015262:Xenobiotics