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Mol Interv. 2009 Jun;9(3):136-45. doi: 10.1124/mi.9.3.7.

Pharmacokinetic assessment of multiple ATP-binding cassette transporters: the power of combination knockout mice.

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Division of Molecular Biology, The Netherlands Cancer Institute, Amsterdam, The Netherlands.


A TP-binding cassette (ABC) multidrug transporters are cellular efflux pumps with broad and often widely overlapping substrate specificities. They can have a major impact on the pharmacokinetics and hence overall pharmacological behavior of many drugs. To study their separate roles and functional overlap, or complementarity, a collection of mice deficient in two or more ABC transporters has been generated. This review discusses recent findings obtained with these models, focusing on pharmacokinetic studies with a number of clinically relevant drugs. In addition, the characterization of these mice and some physiological aspects of ABC multidrug transporters are addressed.

[Indexed for MEDLINE]

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