Systematic Strategy for Developing Glycosyltransferase Inhibitors: Diversity-Oriented Synthesis of FUT8 Inhibitors

Systematic Strategy for Developing Glycosyltransferase Inhibitors: Diversity-Oriented Synthesis of FUT8 Inhibitors Yoshiyuki Manabe , Koki Hizume , Yohei Takakura , Shinji Takamatsu , Eiji Miyoshi , Yoshihiro Kamada , Ramón Hurtado-Guerrero , Koichi Fukase. Synlett, 2023. DOI: 10.1055/a-2221-9096

Glycans control various biological processes depending on their structures. Particularly, core fucose, formed by α1,6-fucosyltransferase (FUT8), has a substantial influence on multiple biological processes. In this study, we investigated the development of FUT8 inhibitors with structural elements encompassing both the glycosyl donor (GDP-fucose) and acceptor (N-glycan) of FUT8. To efficiently optimize the structure of FUT8 inhibitors, we employed a strategy involving fragmentation of the target structure, followed by the structure optimization using diversity-oriented synthesis approaches. This study proposes an efficient strategy to accelerate the structural optimization of middle molecules.

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