Journal
CURRENT DRUG METABOLISM
Volume 11, Issue 7, Pages 603-617Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/138920010792927325
Keywords
Breast cancer resistance protein; BCRP; ATP-binding cassette transporter; ABCG2; multidrug resistance; drug disposition; homology model; mutation analysis
Funding
- National Institutes of Health [GM073715]
- VIP fellowship
- Wellcome Trust [081406/Z/06/Z]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM073715] Funding Source: NIH RePORTER
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The human breast cancer resistance protein (BCRP/ABCG2) is the second member of the G subfamily of the large ATP-binding cassette (ABC) transporter superfamily. BCRP was initially discovered in multidrug resistant breast cancer cell lines where it confers resistance to chemotherapeutic agents such as mitoxantrone, topotecan and methotrexate by extruding these compounds out of the cell. BCRP is capable of transporting non-chemotherapy drugs and xenobiotiocs as well, including nitrofurantoin, prazosin, glyburide, and 2-amino-1-methyl-6-phenylimidazo [4,5-b] pyridine. BCRP is frequently detected at high levels in stem cells, likely providing xenobiotic protection. BCRP is also highly expressed in normal human tissues including the small intestine, liver, brain endothelium, and placenta. Therefore, BCRP has been increasingly recognized for its important role in the absorption, elimination, and tissue distribution of drugs and xenobiotics. At present, little is known about the transport mechanism of BCRP, particularly how it recognizes and transports a large number of structurally and chemically unrelated drugs and xenobiotics. Here, we review current knowledge of structure and function of this medically important ABC efflux drug transporter.
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