The multidrug transporter ABCG2: still more questions than answers.
The multidrug transporter ABCG2: still more questions than answers.
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DOI：
10.1042/bst20160014
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发表时间：
2016-06-15
影响因子：
3.9
通讯作者：
Kerr ID
中科院分区：
文献类型：
--
作者：
Horsey AJ;Cox MH;Sarwat S;Kerr ID
ABCG 2是至少三种人ATP结合盒（ABC）转运蛋白之一，其可以促进多种化学上不相关的药物分子从细胞中输出。这种多药转运能力不仅是化疗中的一个混杂因素，而且也是转运蛋白生物化学中更令人困惑的现象之一。自20世纪最后十年发现ABCG 2以来，有关ABCG 2的定位、生理功能及其广泛的底物范围的许多信息已被揭示。对它的结构和分子机制也有许多研究。在这篇小型综述文章中，我们对ABCG 2采取了拉姆斯菲尔德方法，并基本上询问我们对这种转运蛋白的了解，以及如果我们希望将ABCG 2活性的调节用作治疗方法，我们需要了解这种转运蛋白。
ABCG2 is one of at least three human ATP binding cassette (ABC) transporters which can facilitate the export from cells of a wide range of chemically unrelated drug molecules. This capacity for multidrug transport is not only a confounding factor in chemotherapy, but is also one of the more perplexing phenomena in transporter biochemistry. Since its discovery in the last decade of the 20th century much has been revealed about ABCG2’s localization, physiological function and its broad substrate range. There have also been many investigations of its structure and molecular mechanism. In this mini review article we take a Rumsfeldian approach to ABCG2 and essentially ask what we do know about this transporter, and what we will need to know about this transporter if we wish to use modulation of ABCG2 activity as a therapeutic approach.