Human ABCG2: structure, function, and its role in multidrug resistance.

Human ABCG2: structure, function, and its role in multidrug resistance.
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DOI:
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发表时间:
2012
期刊:
International journal of biochemistry and molecular biology
影响因子:
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通讯作者:
W. Mo;Jian-Ting Zhang
W. Mo;Jian-Ting Zhang
中科院分区:
其他
文献类型:
--
作者:
W. Mo;Jian-Ting Zhang

文献摘要

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Human ABCG2 is a member of the ATP-binding cassette (ABC) transporter superfamily and is known to contribute to multidrug resistance (MDR) in cancer chemotherapy. Among ABC transporters that are known to cause MDR, ABCG2 is particularly interesting for its potential role in protecting cancer stem cells and its complex oligomeric structure. Recent studies have also revealed that the biogenesis of ABCG2 could be modulated by small molecule compounds. These modulators, upon binding to ABCG2, accelerate the endocytosis and trafficking to lysosome for degradation and effectively reduce the half-life of ABCG2. Hence, targeting ABCG2 stability could be a new venue for therapeutic discovery to sensitize drug resistant human cancers. In this report, we review recent progress on understanding the structure, function, biogenesis, as well as physiological and pathophysiological functions of ABCG2.