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High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays

Academic Article
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Overview

related to degree

  • Bryan, Marian C, Ph.D. in Chemistry, Scripps Research 1999 - 2004

authors

  • Bryan, Marian C
  • Lee, L. V.
  • Wong, Chi-Huey

publication date

  • June 2004

journal

  • Bioorganic & Medicinal Chemistry Letters  Journal

abstract

  • A noncovalent carbohydrate microarray was used to screen for possible inhibitors to fucosyltransferases, which are critical to the synthesis of inflammation mediators like sialyl Lewis x (SLe(x)). Inhibition was followed by observation of the transferred fucose on the carbohydrate array with the lectin Tetragonolobus purpureas. Of these compounds, four inhibitors with nanomolar Ki(s) were discovered, with three of the top five inhibitors exhibiting a common architecture.

subject areas

  • Amino Sugars
  • Carbohydrate Sequence
  • Enzyme Inhibitors
  • Fucosyltransferases
  • Kinetics
  • Lotus
  • Molecular Sequence Data
  • Oligosaccharides
  • Plant Lectins
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Research

keywords

  • carbohydrate
  • fucosyltransferase
  • glycoarray
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Identity

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2004.04.001

PubMed ID

  • 15149672
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Additional Document Info

start page

  • 3185

end page

  • 3188

volume

  • 14

issue

  • 12

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