A potent and highly selective sulfotransferase inhibitor

J Am Chem Soc. 2002 Dec 11;124(49):14524-5. doi: 10.1021/ja021086u.

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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adenosine Diphosphate / metabolism
  • Animals
  • Binding, Competitive
  • Combinatorial Chemistry Techniques
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Kinetics
  • Purines / metabolism
  • Purines / pharmacology*
  • Pyrimidines / metabolism
  • Pyrimidines / pharmacology*
  • Rats
  • Sulfotransferases / antagonists & inhibitors*
  • Sulfotransferases / metabolism

Substances

  • Enzyme Inhibitors
  • Purines
  • Pyrimidines
  • Adenosine Diphosphate
  • adenosine 3'-phosphate-5'-phosphate
  • Sulfotransferases
  • tyrosine-ester sulfotransferase