Syntheses of sulfated glycopolymers and analyses of their BACE-1 inhibitory activity

Yuri Nishimura, Hiroki Shudo, Hirokazu Seto, Yu Hoshino, Yoshiko Miura

研究成果: Contribution to journalArticle査読

14 被引用数 (Scopus)

抄録

The glycopolymers for glycosaminoglycan mimic were synthesized, and the inhibitory effects of Alzheimer's β-secretase (BACE-1) were examined. The regio-selective sulfation was conducted on N-acetyl glucosamine (GlcNAc), and the acrylamide derivatives were synthesized with the consequent sulfated GlcNAc. The glycopolymers were synthesized with acrylamide using radical initiator. The glycopolymer with sulfated GlcNAc showed the strong inhibitory effect on BACE-1, and the inhibitory effects were dependent on the sulfation positions. Especially, glycopolymers carrying 3,4,6-O-sulfo-GlcNAc showed the strong inhibitory effect. The docking simulation suggested that glycopolymers bind to the active site of BACE-1.

本文言語英語
ページ(範囲)6390-6395
ページ数6
ジャーナルBioorganic and Medicinal Chemistry Letters
23
23
DOI
出版ステータス出版済み - 12 1 2013

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

フィンガープリント 「Syntheses of sulfated glycopolymers and analyses of their BACE-1 inhibitory activity」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル