Systematic Strategy for the Development of Glycosyltransferase Inhibitors: Diversity-Oriented Synthesis of FUT8 Inhibitors.

This article explores the development of glycosyltransferase inhibitors, specifically focusing on FUT8 inhibitors. FUT8 is an enzyme that plays a crucial role in various biological processes. The researchers used diversity-oriented synthesis (DOS) to create compound libraries of FUT8 inhibitors. Through late-stage functionalization and the combination of glycosyl donor and acceptor mimics, they successfully developed a FUT8 inhibitor. The study also discusses the modification of guanine derivatives and the creation of bi-substrate mimics, which are expected to exhibit exceptional selectivity among FUTs. Overall, this article presents an efficient methodology for optimizing the structure of middle molecules. [Extracted from the article]