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Small Molecule Screening for Inhibitors of the YopH Phosphatase of Yersinia pseudotuberculosis

  • Jonas Eriksson
  • Christin Grundström
  • A. Elisabeth Sauer-Eriksson
  • Uwe H. Sauer
  • Hans Wolf-Watz
  • Mikael ElofssonEmail author
Conference paper
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 954)

Abstract

Bacterial virulence systems are attractive targets for development of new antibacterial agents. Yersinia spp. utilize the type III secretion (T3S) system to secrete and translocate Yersinia outer proteins (Yop effectors) into the cytosol of the target cell and thereby overcome host defenses to successfully establish an infection. Thus, the Yop effectors constitute attractive targets for drug development. In the present study we apply small molecule screening to identify inhibitors of one of the secreted proteins YopH, a tyrosine phosphatase required for virulence. Characterization of seven inhibitors indicated that both competitive and noncompetitive inhibitors were identified with IC50 values of 6–20 μM.

Keywords

Effector Protein Small Organic Molecule Yersinia Enterocolitica Yersinia Pestis Protein Tyrosine Phosphatase Inhibitor 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Notes

Acknowledgments

We are grateful for support from the Kempe Foundations, the Carl Trygger’s Foundation, Umea City, the Swedish Research Council, the Knut and Alice Wallenberg Foundation, and the Swedish Governmental Agency for Innovation Systems (VINNOVA).

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Copyright information

© Springer Science+Business Media New York 2012

Authors and Affiliations

  • Jonas Eriksson
    • 1
    • 2
  • Christin Grundström
    • 2
    • 3
  • A. Elisabeth Sauer-Eriksson
    • 2
    • 3
  • Uwe H. Sauer
    • 2
    • 3
  • Hans Wolf-Watz
    • 3
    • 4
  • Mikael Elofsson
    • 2
    • 3
    • 5
    Email author
  1. 1.Laboratories for Chemical BiologyUmeå UniversityUmeåSweden
  2. 2.Department of ChemistryUmeå UniversityUmeåSweden
  3. 3.Umeå Centre for Microbial Research (UCMR)Umeå UniversityUmeåSweden
  4. 4.Department of Molecular BiologyUmeå UniversityUmeåSweden
  5. 5.Molecular Infection Medicine Sweden (MIMS)Umeå UniversityUmeåSweden

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