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

DOI PDF 参考文献47件
  • Yoshiyuki Manabe
    Department of Chemistry, Graduate School of Science, Osaka University
  • Koichi Fukase
    Department of Chemistry, Graduate School of Science, Osaka University
  • Koki Hizume
    Department of Chemistry, Graduate School of Science, Osaka University
  • Yohei Takakura
    Department of Chemistry, Graduate School of Science, Osaka University
  • Shinji Takamatsu
    Department of Molecular Biochemistry and Clinical Investigation, Graduate School of Medicine, Osaka University
  • Eiji Miyoshi
    Department of Molecular Biochemistry and Clinical Investigation, Graduate School of Medicine, Osaka University
  • Yoshihiro Kamada
    Department of Advanced Metabolic Hepatology, Graduate School of Medicine, Osaka University
  • Ramón Hurtado-Guerrero
    Institute of Biocomputation and Physics of Complex Systems (BIFI), University of Zaragoza

書誌事項

公開日
2023-12-04
資源種別
journal article
DOI
  • 10.1055/a-2221-9096
公開者
Georg Thieme Verlag KG

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説明

<jats:title>Abstract</jats:title><jats:p>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 a structure optimization using a diversity-oriented synthesis approach. This study proposes an efficient strategy to accelerate the structural optimization of middle molecules.</jats:p>

収録刊行物

  • Synlett

    Synlett 2023-12-04

    Georg Thieme Verlag KG

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