State Key Laboratory and Institute of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin, 300071, P. R. China.
State Key Laboratory of Natural and Biomimetic Drugs, Chemical Biology Center State Key Laboratory of Natural and Biomimetic Drugs, Chemical Biology Center, and, School of Pharmaceutical Sciences, Peking University, Beijing, 100191, P. R. China.
Chembiochem. 2023 Jan 3;24(1):e202200388. doi: 10.1002/cbic.202200388. Epub 2022 Sep 7.
N-Glycosylation is often essential for the structure and function of proteins. However, N-glycosylated proteins from natural sources exhibit considerable heterogeneity in the appended oligosaccharides, bringing daunting challenges to corresponding basic research and therapeutic applications. To address this issue, various synthetic, enzymatic, and chemoenzymatic approaches have been elegantly designed. Utilizing the endoglycosidase-catalyzed transglycosylation method, a single N-acetylglucosamine (N-GlcNAc, analogous to a tree stump) on proteins can be converted to various homogeneous N-glycosylated forms, thereby becoming the focus of research efforts. In this concept article, we briefly introduce the methods that allow the generation of N-GlcNAc and its close analogues on proteins and peptides and highlight the current challenges and opportunities the scientific community is facing.
N-糖基化通常对蛋白质的结构和功能至关重要。然而，天然来源的 N-糖基化蛋白在附加的寡糖上表现出相当大的异质性，给相应的基础研究和治疗应用带来了巨大的挑战。为了解决这个问题，已经设计了各种合成、酶和化学酶方法。利用内切糖苷酶催化的转糖基化方法，蛋白质上的单个 N-乙酰葡萄糖胺（N-GlcNAc，类似于树桩）可以转化为各种同质的 N-糖基化形式，因此成为研究的焦点。在这篇概念文章中，我们简要介绍了在蛋白质和肽上生成 N-GlcNAc 及其类似物的方法，并强调了科学界目前面临的挑战和机遇。
