Chapter 29. Small Molecule Inhibitors of the Sulfotransferases

  1. Prof. Dr. Chi-Huey Wong
  1. Dawn E. Verdugo,
  2. Lars C. Pedersen,
  3. Carolyn R. Bertozzi

Published Online: 28 JAN 2005

DOI: 10.1002/3527602437.ch29

Book Title

Carbohydrate-Based Drug Discovery

Carbohydrate-Based Drug Discovery

Additional Information

How to Cite

Verdugo, D. E., Pedersen, L. C. and Bertozzi, C. R. (2005) Small Molecule Inhibitors of the Sulfotransferases, in Carbohydrate-Based Drug Discovery (ed C.-H. Wong), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527602437.ch29

Editor Information

  1. Ernest W. Hahn Chair in Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines RoadLa Jolla, CA 92037, USA

Publication History

  1. Published Online: 28 JAN 2005
  2. Published Print: 26 AUG 2003

ISBN Information

Print ISBN: 9783527306329

Online ISBN: 9783527602438

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CHAPTER TOOLS

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Keywords:

  • sulfotransferases;
  • small molecule inhibitors;
  • sulfation;
  • EST as a model;
  • ST for inhibitor design;
  • assays for screening of STs

Summary

  • Introduction: Sulfotransferases and the Biology of Sulfation

  • EST as a Model ST for Inhibitor Design

    • Inhibitors of EST Targeted Toward the PAPS Binding Site

    • A Bisubstrate Analogue Approach to EST Inhibition

    • Discovery of EST Inhibitors from a Library of PAP Analogues

    • Inhibition of EST by Dietary Agents and Environmental Toxins

  • Inhibition of Representative Golgi-Resident Sulfotransferases: GST-2, GST-3, and TPST-2

    • Heterocyclic Inhibitors of GST-2 and GST-3

    • Tethered Inhibitors of TPST-2

  • Assays for High-Throughput Screening of STs

    • A Continuous ST Assay

    • Immobilized Enzyme Mass Spectrometry (IEMS) Assay

    • A 96-Well Direct Capture ‘Dot-Blot’ Assay for Carbohydrate STs

  • New Directions in Inhibitor Discovery

  • Conclusions

  • Acknowledgements

  • References

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