Elsevier

Kidney International

Volume 73, Issue 2, 2 January 2008, Pages 220-225
Kidney International

Original Article
The breast cancer resistance protein transporter ABCG2 is expressed in the human kidney proximal tubule apical membrane

https://doi.org/10.1038/sj.ki.5002645Get rights and content
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The Breast Cancer Resistance Protein (BCRP/ABCG2) is a transporter restricting absorption and enhancing excretion of many compounds including anticancer drugs. This transporter is highly expressed in many tissues; however, in human kidney, only the mRNA was found in contrast to the mouse kidney, where the transporter is abundant. In bcrp/abcg2(−/−) mice, the expression of two sterol transporter genes, abcg5 and abcg8, was strongly increased in the kidney, perhaps as a compensatory mechanism to upregulate efflux. We found using immunohistochemical analysis clear localization of BCRP/ABCG2 to the proximal tubule brush border membrane of the human kidney comparable to that of other ABC transporters such as P-glycoprotein/ABCB1, MRP2/ABCC2, and MRP4/ABCC4. Hoechst 33342 dye efflux from primary human proximal tubule cells was significantly reduced by the BCRP/ABCG2 inhibitors fumitremorgin C and nelfinavir. Our study shows that in addition to other apical ABC transporters, BCRP/ABCG2 may be important in renal drug excretion.

KEYWORDS

ABC transporter
cell and transport physiology
drug excretion
immunostaining

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3

These authors contributed equally to this work.