bcrp - publications

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1. Drug Metab Dispos. 2012 Mar 8. [Epub ahead of print]

Quantitative Proteomics of Transporter Expression in Brain Capillary Endothelial
Cells Isolated from P-gp, BCRP, and P-gp/BCRP Knockout Mice.

Agarwal S, Uchida Y, Mittapalli RK, Sane R, Terasaki T, Elmquist WF.

1 University of Minnesota;

The objective of this study was to quantitatively examine the protein expression
of relevant transporters and other proteins in the brain capillary endothelial
cells isolated from wild-type mice, and P-gp, Bcrp, and P-gp/Bcrp knockout mice.
Following the isolation of brain capillary endothelial cells, a highly sensitive
liquid chromatography-tandem mass spectrometry method (LC/MS/MS) with multiple
reaction monitoring was employed to determine the quantitative expression of
membrane transporters at the blood-brain barrier of the various mouse genotypes.
Quantitative expression of 29 protein molecules, including 12 ABC transporters,
10 SLC transporters, 5 receptors and 2 house-keeping proteins were examined by
quantitative proteomics in the four mouse genotypes. There was no significant
difference in the expression of P-gp between the wild-type and Bcrp1-/- mice.
Similarly, BCRP expression was not significantly different between the wild-type
and Mdr1a/b-/- mice. There was no significant difference in the expression of any
of the measured proteins in the brain capillary endothelial cells across the
genotypes, except for the lack of expression of the corresponding protein in the
mice that had a genetic deletion of P-gp or BCRP. In conclusion, using a
quantitative proteomic approach, we have shown that there are no changes in the
expression of several relevant transporters in brain capillary endothelial cells
isolated from single and combination knockout mice. These data suggest that the
mechanism behind the functional compensation between P-gp and BCRP at the BBB is
not related to compensatory changes in transporter expression.

PMID: 22401960 [PubMed - as supplied by publisher]