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A potent and highly selective sulfotransferase inhibitor

Academic Article
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Overview

related to degree

  • Ding, Sheng, Ph.D. in Chemistry, Scripps Research 1999 - 2003
  • Chapman, Eli, Ph.D. in Chemistry, Scripps Research , Transferred from Columbia University 1998 - 2002

authors

  • Chapman, Eli
  • Ding, Sheng
  • Schultz, Peter
  • Wong, Chi-Huey

publication date

  • December 2002

journal

  • Journal of the American Chemical Society  Journal

abstract

  • In the present work, we have used a newly developed, fluorescence-based assay to screen a library of >30 000 compounds as potential beta-arylsulfotransferase-IV inhibitors. A total of 11 inhibitors were discovered. Most of the compounds discovered showed low micromolar inhibition, but one of the compounds showed potent inhibition (Ki = 96 nM). The most potent of these inhibitors was tested against a variety of other purine binding enzymes and showed remarkable specificity.

subject areas

  • Adenosine Diphosphate
  • Animals
  • Binding, Competitive
  • Combinatorial Chemistry Techniques
  • Enzyme Inhibitors
  • Kinetics
  • Purines
  • Pyrimidines
  • Rats
  • Sulfotransferases
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Identity

International Standard Serial Number (ISSN)

  • 0002-7863

Digital Object Identifier (DOI)

  • 10.1021/ja021086u

PubMed ID

  • 12465948
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Additional Document Info

start page

  • 14524

end page

  • 14525

volume

  • 124

issue

  • 49

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