Innentitelbild: Development of a FUT8 Inhibitor with Cellular Inhibitory Properties (Angew. Chem. 52/2024)

Core fucosylation, catalyzed by α‐1,6‐fucosyltransferase (FUT8), is implicated in various diseases, making FUT8 inhibitors highly desirable. In their Research Article (e202414682), Yoshiyuki Manabe, Koichi Fukase et al. developed FUT8 inhibitors with potent cellular activity. Through high‐throughput screening and structural optimization, potent FUT8 inhibitors were identified. Additionally, prodrug derivatization enhanced the stability of these inhibitors, enabling the suppression of core fucose expression in cell‐based assays.