Rebbeor J F, Connolly G C, Dumont M E, Ballatori N
Department of Environmental Medicine, University of Rochester, School of Medicine, Rochester, NY 14642, USA.
Biochem J. 1998 Sep 15;334 ( Pt 3)(Pt 3):723-9. doi: 10.1042/bj3340723.
Turnover of cellular reduced glutathione (GSH) is accomplished predominantly by export into the extracellular space; however, the plasma membrane transport mechanisms that mediate GSH efflux are not well characterized. The present study examined GSH transport using secretory vesicles isolated from the sec6-4 mutant strain of Saccharomyces cerevisiae. In contrast with studies in mammalian membrane vesicles, GSH transport in yeast secretory vesicles was mediated largely by an ATP-dependent, low-affinity pathway (Km 19+/-5 mM). ATP-dependent [3H]GSH transport was cis-inhibited by substrates of the yeast YCF1 transporter, including sulphobromophthalein, glutathione S-conjugates and the alkaloid verapamil, and was competitively inhibited by S-(2, 4-dinitrophenyl)glutathione (DNP-SG). Similarly, GSH competitively inhibited ATP-dependent [3H]DNP-SG transport, with a Ki of 18+/-2 mM, but had no effect on ATP-dependent [3H]taurocholate transport. ATP-dependent GSH transport was not affected by either membrane potential or pH-gradient uncouplers, but was inhibited by 4, 4'-di-isothiocyanatostilbene-2,2'-disulphonate, probenecid and sulphinpyrazone, which are inhibitors of mrp1 and mrp2, mammalian homologues of the yeast YCF1 transporter. Western blot analysis of the secretory vesicle membrane fraction confirmed the presence of Ycf1p. These results provide the first direct evidence for low-affinity, ATP-dependent transport of GSH, and demonstrate that this ATP-dependent pathway displays kinetic characteristics similar to those of the yeast YCF1 transporter.
细胞内还原型谷胱甘肽(GSH)的周转主要通过向细胞外空间输出完成;然而,介导GSH外排的质膜转运机制尚未得到充分表征。本研究使用从酿酒酵母sec6 - 4突变株分离的分泌囊泡来检测GSH转运。与哺乳动物膜囊泡的研究不同,酵母分泌囊泡中的GSH转运主要由一种ATP依赖的低亲和力途径介导(Km为19±5 mM)。ATP依赖的[³H]GSH转运被酵母YCF1转运体的底物顺式抑制,包括磺溴酞、谷胱甘肽S - 共轭物和生物碱维拉帕米,并被S -(2,4 - 二硝基苯基)谷胱甘肽(DNP - SG)竞争性抑制。同样,GSH竞争性抑制ATP依赖的[³H]DNP - SG转运,Ki为18±2 mM,但对ATP依赖的[³H]牛磺胆酸盐转运没有影响。ATP依赖的GSH转运不受膜电位或pH梯度解偶联剂的影响,但被4,4'-二异硫氰酸根合芪 - 2,2'-二磺酸盐、丙磺舒和磺吡酮抑制,这些是酵母YCF1转运体的哺乳动物同源物mrp1和mrp2的抑制剂。分泌囊泡膜组分的蛋白质免疫印迹分析证实了Ycf1p的存在。这些结果为GSH的低亲和力、ATP依赖转运提供了首个直接证据,并表明这种ATP依赖途径显示出与酵母YCF1转运体相似的动力学特征。