Higgins C F, Gottesman M M
Imperial Cancer Research Fund Laboratories, University of Oxford, John Radcliffe Hospital, UK.
Trends Biochem Sci. 1992 Jan;17(1):18-21. doi: 10.1016/0968-0004(92)90419-a.
The phenomenon of multidrug resistance is correlated with the presence of a membrane protein, P-glycoprotein, which pumps a wide variety of drugs out of cells thus reducing their toxicity. However, the mechanism of this pumping action remains unclear. In this article, we suggest that several properties of the multidrug transporter may be explained if it acts as a 'flippase' to transport drugs from the inner leaflet of the lipid bilayer to the outer or to the external medium.
多药耐药现象与一种膜蛋白——P-糖蛋白的存在相关,该蛋白能将多种药物泵出细胞,从而降低其毒性。然而,这种泵浦作用的机制仍不清楚。在本文中,我们提出,如果多药转运蛋白作为一种“翻转酶”,将药物从脂质双分子层的内层转运到外层或细胞外介质中,那么多药转运蛋白的几个特性或许可以得到解释。