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Rapid discovery of potent sulfotransferase inhibitors by diversity-oriented reaction in microplates followed by in situ screening

Academic Article
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Overview

related to degree

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

authors

  • Best, M. D.
  • Brik, A.
  • Chapman, Eli
  • Lee, L. V.
  • Cheng, W. C.
  • Wong, Chi-Huey

publication date

  • June 2004

journal

  • ChemBioChem  Journal

abstract

  • Rapid diversity-oriented microplate library synthesis and in situ screening with a high-throughput fluorescence-based assay were used to develop potent inhibitors of beta-arylsulfotransferase IV (beta-AST-IV). This strategy leads to facile inhibitor synthesis and study as it allows protecting-group manipulation and product isolation from other library components to be avoided. Through repeated library formation, three aspects of inhibitor makeup, the identities of the two binding groups and the length of the linker between them, were independently optimized. Several potent inhibitors were obtained, one of which was determined to have an inhibition constant K(i) of 5 nM. This compound is the most potent beta-AST-IV inhibitor developed to date, with a K(i) value more than five orders of magnitude lower than the Michaelis constant K(m) for the substrate whose binding it inhibits.

subject areas

  • Binding Sites
  • Catalysis
  • Combinatorial Chemistry Techniques
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors
  • Fluorescence
  • Spectrometry, Mass, Electrospray Ionization
  • Structure-Activity Relationship
  • Sulfotransferases
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Research

keywords

  • combinatorial chemistry
  • enzymes
  • high-throughput screening
  • inhibitors
  • sulfotransferases
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Identity

International Standard Serial Number (ISSN)

  • 1439-4227

Digital Object Identifier (DOI)

  • 10.1002/cbic.200300841

PubMed ID

  • 15174164
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Additional Document Info

start page

  • 811

end page

  • 819

volume

  • 5

issue

  • 6

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