Ma D, Russell D G, Beverley S M, Turco S J
Department of Biochemistry, University of Kentucky Medical Center, Lexington, Kentucky 40536, USA.
J Biol Chem. 1997 Feb 7;272(6):3799-805.
The synthesis of glycoconjugates within the secretory pathway of eukaryotes requires the provision of lumenal nucleotide-sugar substrates. This is particularly important for eukaryotic microbes such as Leishmania because they must synthesize considerable amounts of extracellular and cell surface glycoconjugates that play significant roles in the infectious cycle. Here we used properly oriented sealed microsomes to characterize lumenal uptake of GDP-Man in Leishmania donovani. In this system, GDP-Man uptake was saturable with an apparent Km for GDP-Man of 0.3 microM and facilitated its use as a donor substrate for lipophosphoglycan (LPG) synthesis. A lpg2(-) deletion mutant showed loss of GDP-Man but not UDP-Gal uptake, which was restored by introduction of the gene LPG2. Immunoelectron microscopy localized an active, epitope-tagged LPG2 protein to the Golgi apparatus. Thus, LPG2 is required for nucleotide-sugar transport activity and probably encodes this Golgi transporter. LPG2 belongs to a large family of eukaryotic genes that potentially encode transporters with different substrate specificities and/or cellular locations. In the future, the amenability of the Leishmania system to biochemical and genetic manipulation will assist in functional characterization of nucleotide-sugar transports from this and other eukaryotes. Furthermore, since LPG2 plays an important role in the Leishmania infectious cycle and mammalian cells lack a Golgi GDP-Man transporter, this activity may offer a new target for chemotherapy.
真核生物分泌途径中糖缀合物的合成需要提供腔内核苷酸糖底物。这对利什曼原虫等真核微生物尤为重要,因为它们必须合成大量在感染周期中起重要作用的细胞外和细胞表面糖缀合物。在这里,我们使用正确定向的密封微粒体来表征杜氏利什曼原虫中GDP-甘露糖的腔内摄取。在这个系统中,GDP-甘露糖的摄取是可饱和的,其对GDP-甘露糖的表观Km为0.3微摩尔,并促进其作为脂磷壁酸聚糖(LPG)合成的供体底物。一个lpg2(-)缺失突变体显示GDP-甘露糖摄取丧失,但UDP-半乳糖摄取未丧失,通过引入基因LPG2可恢复。免疫电子显微镜将一种有活性的、带有表位标签的LPG2蛋白定位到高尔基体。因此,LPG2是核苷酸糖转运活性所必需的,可能编码这种高尔基体转运蛋白。LPG2属于一个大型真核基因家族,可能编码具有不同底物特异性和/或细胞定位的转运蛋白。未来,利什曼原虫系统对生化和基因操作的适应性将有助于对来自该真核生物和其他真核生物的核苷酸糖转运进行功能表征。此外,由于LPG2在利什曼原虫感染周期中起重要作用,而哺乳动物细胞缺乏高尔基体GDP-甘露糖转运蛋白,这种活性可能为化疗提供一个新靶点。