Xing Ling; Sixiu Liu; Yixuan Yang; Qian Dong; Lisa A. Marcaurelle; Wei Huang; Yun Ding; Xuan Wang; Xiaojie Lu
Bioconjugate Chem., 2023, 34(4), 616-620
https://doi.org/10.1021/acs.bioconjchem.3c00068

Abstract

Carbohydrates are an important class of naturally active products and play vital roles in regulating various physiological activities. To meet the demand for carbohydrate-based libraries used for the identification of potential drug candidates for pharmaceutical-related targets, we developed a set of on-DNA protocols to construct the DNA-encoded glycoconjugates, including Seyferth-Gilbert homologation, anomeric azidation, and CuAAC cyclization. These on-DNA chemistries enable the generation and modification of DNA-linked glycosyl compounds with good conversions and broad substrate scope. Finally, three DNA-linked glycoconjugate libraries were successfully generated to demonstrate their applicability and feasibility in library preparation.