Newstead Simon, Parker Joanne, Deme Justin, Feddersen Bjarne, Lea Susan
Res Sq. 2025 Aug 5:rs.3.rs-7213965. doi: 10.21203/rs.3.rs-7213965/v1.
GDP-Mannose transporters are Golgi-localised solute carriers that are essential for the virulence of pathogenic fungi, serving as critical components of fungal glycosylation pathways. However, the mechanism by which nucleotide sugars are recognised and transported across the Golgi membrane remains unclear, hindering efforts to develop effective inhibitors that could serve as novel antifungal agents. Here, we present cryo-EM structures of the GDP-Mannose transporter, Vrg4, from Candida albicans in complex with nanobodies and in both the cytoplasmic and Golgi-facing states. Structural comparisons between these two states, in addition to a GDP-mannose bound structure, demonstrate the importance of ligand movement during transport. Additionally, we demonstrate the ability of the nanobodies to specifically inhibit Vrg4, presenting proof-of-principle that nanobodies can be used as effective inhibitors of nucleotide sugar transport and glycosylation in cells.
GDP-甘露糖转运蛋白是定位于高尔基体的溶质载体,对致病真菌的毒力至关重要,是真菌糖基化途径的关键组成部分。然而,核苷酸糖如何被识别并跨高尔基体膜运输的机制仍不清楚,这阻碍了开发可作为新型抗真菌剂的有效抑制剂的努力。在此,我们展示了白色念珠菌的GDP-甘露糖转运蛋白Vrg4与纳米抗体结合时在细胞质和高尔基体朝向状态下的冷冻电镜结构。这两种状态之间的结构比较,以及GDP-甘露糖结合结构,证明了配体在运输过程中移动的重要性。此外,我们证明了纳米抗体特异性抑制Vrg4的能力,提供了纳米抗体可作为细胞内核苷酸糖运输和糖基化有效抑制剂的原理证明。