1. The breast cancer resistance protein transporter ABCG2 is expressed in the human kidney proximal tubule apical membrane
- Author
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Suzanne Heemskerk, Rachel Sayer, Colin D.A. Brown, Miriam Huls, Amy S. Windass, Rosalinde Masereeuw, Frans G. M. Russel, and J. J. M. W. van den Heuvel
- Subjects
medicine.medical_specialty ,animal structures ,Abcg2 ,Membrane transport and intracellular motility [NCMLS 5] ,cell and transport physiology ,ATP-binding cassette transporter ,Synthetic Organic Chemistry ,ABCC4 ,Polymerase Chain Reaction ,Kidney Tubules, Proximal ,Metabolism, transport and motion [NCMLS 2] ,Mice ,Internal medicine ,medicine ,ATP Binding Cassette Transporter, Subfamily G, Member 2 ,Animals ,Humans ,RNA, Messenger ,Renal disorder [IGMD 9] ,immunostaining ,Kidney ,biology ,Multidrug resistance-associated protein 2 ,Cell Membrane ,Transporter ,Apical membrane ,Immunohistochemistry ,Molecular biology ,Multidrug Resistance-Associated Protein 2 ,Neoplasm Proteins ,Rats ,Renal disorders [UMCN 5.4] ,medicine.anatomical_structure ,Endocrinology ,drug excretion ,Nephrology ,biology.protein ,ATP-Binding Cassette Transporters ,ABC transporter ,Efflux - Abstract
Contains fulltext : 70782.pdf (Publisher’s version ) (Closed access) 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. more...
- Published
- 2008
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