Department of Urology, Boston Children's Hospital, Boston, Massachusetts, United States of America.
Department of Surgery, Harvard Medical School, Boston, Massachusetts, United States of America.
PLoS Biol. 2018 Nov 27;16(11):e2006951. doi: 10.1371/journal.pbio.2006951. eCollection 2018 Nov.
Glycosylation is a fundamental modification of proteins and membrane lipids. Toxins that utilize glycans as their receptors have served as powerful tools to identify key players in glycosylation processes. Here, we carried out Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR)-Cas9-mediated genome-wide loss-of-function screens using two related bacterial toxins, Shiga-like toxins (Stxs) 1 and 2, which use a specific glycolipid, globotriaosylceramide (Gb3), as receptors, and the plant toxin ricin, which recognizes a broad range of glycans. The Stxs screens identified major glycosyltransferases (GTs) and transporters involved in Gb3 biosynthesis, while the ricin screen identified GTs and transporters involved in N-linked protein glycosylation and fucosylation. The screens also identified lysosomal-associated protein transmembrane 4 alpha (LAPTM4A), a poorly characterized four-pass membrane protein, as a factor specifically required for Stxs. Mass spectrometry analysis of glycolipids and their precursors demonstrates that LAPTM4A knockout (KO) cells lack Gb3 biosynthesis. This requirement of LAPTM4A for Gb3 synthesis is not shared by its homolog lysosomal-associated protein transmembrane 4 beta (LAPTM4B), and switching the domains between them determined that the second luminal domain of LAPTM4A is required, potentially acting as a specific "activator" for the GT that synthesizes Gb3. These screens also revealed two Golgi proteins, Transmembrane protein 165 (TMEM165) and Transmembrane 9 superfamily member 2 (TM9SF2), as shared factors required for both Stxs and ricin. TMEM165 KO and TM9SF2 KO cells both showed a reduction in not only Gb3 but also other glycosphingolipids, suggesting that they are required for maintaining proper levels of glycosylation in general in the Golgi. In addition, TM9SF2 KO cells also showed defective endosomal trafficking. These studies reveal key Golgi proteins critical for regulating glycosylation and glycolipid synthesis and provide novel therapeutic targets for blocking Stxs and ricin toxicity.
糖基化是蛋白质和膜脂的基本修饰。利用聚糖作为受体的毒素已成为鉴定糖基化过程中关键因子的有力工具。在这里,我们使用两种相关的细菌毒素,即类志贺毒素(Stx)1 和 2,以及植物毒素蓖麻毒素,进行了基于 Clustered Regularly Interspaced Short Palindromic Repeats(CRISPR)-Cas9 的全基因组功能丧失筛选。Stx 利用特定的糖脂,即神经节苷脂 Gb3,作为受体,而蓖麻毒素则识别广泛的聚糖。Stx 筛选鉴定了参与 Gb3 生物合成的主要糖基转移酶(GT)和转运蛋白,而蓖麻毒素筛选鉴定了参与 N-连接蛋白糖基化和岩藻糖基化的 GT 和转运蛋白。筛选还鉴定了溶酶体相关蛋白跨膜 4α(LAPTM4A),一种特征描述较差的四跨膜蛋白,是 Stx 所必需的因素。糖脂及其前体的质谱分析表明,LAPTM4A 敲除(KO)细胞缺乏 Gb3 生物合成。LAPTM4A 对 Gb3 合成的这种需求与其同源物溶酶体相关蛋白跨膜 4β(LAPTM4B)不同,并且在它们之间切换结构域确定了 LAPTM4A 的第二个内腔结构域是必需的,可能充当合成 Gb3 的 GT 的特异性“激活剂”。这些筛选还揭示了两种高尔基体蛋白,跨膜蛋白 165(TMEM165)和跨膜 9 超家族成员 2(TM9SF2),是 Stx 和蓖麻毒素都需要的共同因子。TMEM165 KO 和 TM9SF2 KO 细胞不仅 Gb3 减少,而且其他糖脂减少,表明它们对于维持高尔基体中一般糖基化的适当水平是必需的。此外,TM9SF2 KO 细胞还显示出内体运输缺陷。这些研究揭示了调控糖基化和糖脂合成的关键高尔基体蛋白,并为阻断 Stx 和蓖麻毒素毒性提供了新的治疗靶点。