Cowman A F, Karcz S, Galatis D, Culvenor J G
Walter and Eliza Hall Institute of Medical Research, Melbourne Victoria, Australia.
J Cell Biol. 1991 Jun;113(5):1033-42. doi: 10.1083/jcb.113.5.1033.
Resistance to chloroquine in Plasmodium falciparum bears a striking similarity to the multi-drug resistance (MDR) phenotype of mammalian tumor cells which is mediated by overexpression of P-glycoprotein. We show here that the P. falciparum homologue of the P-glycoprotein (Pgh1) is a 160,000-D protein that is expressed throughout the asexual erythrocytic life cycle of the parasite. Quantitative immunoblotting analysis has shown that the protein is expressed at approximately equal levels in chloroquine resistant and sensitive isolates suggesting that overexpression of Pgh1 is not essential for chloroquine resistance. The chloroquine-resistant cloned line FAC8 however, does express approximately threefold more Pgh1 protein than other isolates which is most likely because of the increased pfmdr1 gene copy number present in this isolate. Immunofluorescence and immunoelectron microscopy has demonstrated that Pgh1 is localized on the membrane of the digestive vacuole of mature parasites. This subcellular localization suggests that Pgh1 may modulate intracellular chloroquine concentrations and has important implications for the normal physiological function of this protein.
恶性疟原虫对氯喹的耐药性与哺乳动物肿瘤细胞的多药耐药(MDR)表型有着惊人的相似性,后者是由P-糖蛋白的过表达介导的。我们在此表明,P-糖蛋白(Pgh1)的恶性疟原虫同源物是一种160,000道尔顿的蛋白质,在该寄生虫的无性红细胞生命周期中均有表达。定量免疫印迹分析表明,该蛋白在氯喹耐药和敏感分离株中的表达水平大致相等,这表明Pgh1的过表达对于氯喹耐药性并非必不可少。然而,耐氯喹的克隆系FAC8表达的Pgh1蛋白比其他分离株大约多三倍,这很可能是因为该分离株中存在的pfmdr1基因拷贝数增加。免疫荧光和免疫电子显微镜已证明,Pgh1定位于成熟寄生虫消化液泡的膜上。这种亚细胞定位表明,Pgh1可能调节细胞内氯喹浓度,并且对该蛋白的正常生理功能具有重要意义。