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[摘要]：Breast cancer resistance protein (BCRP, MXR, ABCG2) is a well-known protein related to acute myeloid leukemia (AML) resistance to chemotherapeutic treatments. This protein is a member of the ATP-binding cassette family which to date comprises 48 members. BCRP is able to efflux mitoxantrone, anthracyclines, taxoids; and methotrexate, as well as topoisomerase I inhibitors. BCRP function can easily be evaluated by anticancer drug uptake. This uptake can be directly followed by flow cytometry or indirectly by cytotoxic assays. A variety of BCRP inhibitors have been described which are more or less specific and active. Despite the great variety of BCRP inhibitors available, the use of these agents in therapy has not fulfilled its promise, at least concerning solid tumors. This article reviews the state of the art of BCRP inhibitors and attempts to draw conclusions related to the potential clinical use of these compounds. |
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