Synthesis of a bisubstrate-type inhibitor of N- acetylglucosaminyltransferases

Shinya Hanashima, Shino Manabe, Kei Ichiro Inamori, Naoyuki Taniguchi, Yukishige Ito

Research output: Contribution to journalArticlepeer-review

21 Citations (Scopus)

Abstract

Transfer interference: Synthesis of the bisubstrate-type N-acetylglucosaminyltransferase (GnT) inhibitor 1 was achieved by a polymer-resin hybrid capture-release strategy for the construction of the acceptor component. One-pot ligation in aqueous media produced the coupling product, and subsequent construction of a diphosphate linkage led to 1. Inhibitory activities toward GnT-V and GnT-IX were evaluated and revealed the potency of 1 toward the latter enzyme.

Original languageEnglish
Pages (from-to)5674-5677
Number of pages4
JournalAngewandte Chemie - International Edition
Volume43
Issue number42
DOIs
Publication statusPublished - 2004 Oct 25
Externally publishedYes

Keywords

  • Bisubstrates
  • Glycoproteins
  • Inhibitors
  • Solid-phase synthesis
  • Transferases

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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