Synthesis of low-molecular weight fucoidan derivatives and their binding abilities to SARS-CoV-2 spike proteins

Tatsuki Koike, Aoi Sugimoto, Shuhei Kosono, Sumika Komaba, Yuko Kanno, Takashi Kitamura, Itsuki Anzai, Tokiko Watanabe, Daisuke Takahashi, Kazunobu Toshima

研究成果: Article査読

1 被引用数 (Scopus)

抄録

Fucoidan derivatives10-13, whose basic sugar chains are composed of repeating α(1,4)-linkedl-fucopyranosyl residues with different sulfation patterns, were designed and systematically synthesized. A structure-activity relationship (SAR) study examined competitive inhibition by thirteen fucoidan derivatives against heparin binding to the SARS-CoV-2 spike (S) protein. The results showed for the first time that10exhibited the highest inhibitory activity of the fucoidan derivatives used. The inhibitory activity of10was much higher than that of fondaparinux, the reported ligand of SARS-CoV-2 S protein. Furthermore,10exhibited inhibitory activities against the binding of heparin with several mutant SARS-CoV-2 S proteins, but was found to not inhibit factor Xa (FXa) activity that could otherwise lead to undesirable anticoagulant activity.

本文言語English
ページ(範囲)2016-2021
ページ数6
ジャーナルRSC Medicinal Chemistry
12
12
DOI
出版ステータスPublished - 2021 12月

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 薬理学
  • 薬科学
  • 創薬
  • 有機化学

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