Horsey Aaron J, Cox Megan H, Sarwat Sunehera, Kerr Ian D
School of Life Sciences, University of Nottingham, Queens Medical Centre, Nottingham NG7 2UH, U.K.
Biochem Soc Trans. 2016 Jun 15;44(3):824-30. doi: 10.1042/BST20160014.
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.
ABCG2是人类至少三种ATP结合盒（ABC）转运蛋白之一，它能够促进多种化学结构不相关的药物分子从细胞中排出。这种多药转运能力不仅是化疗中的一个混杂因素，也是转运蛋白生物化学中较令人困惑的现象之一。自20世纪最后十年被发现以来，关于ABCG2的定位、生理功能及其广泛的底物范围已揭示了很多信息。对其结构和分子机制也进行了许多研究。在这篇小型综述文章中，我们采用拉姆斯菲尔德式的方法来探讨ABCG2，本质上是问我们对这种转运蛋白了解多少，以及如果我们希望将调节ABCG2活性作为一种治疗方法，我们还需要了解关于这种转运蛋白的哪些方面。
