The Path from Target Validation to the Clinic
  • Mohammed Sajid
  • Stephanie A. Robertson
  • Linda S. Brinen
  • James H. McKerrow
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 712)


Cruzain is the major papain-like cysteine protease of Trypanosoma cruzi, the etiological agent causing Chagas’ disease in humans in South America. Cruzain is indispensable for the survival and propagation of this protozoan parasite and therefore, it has attracted considerable interest as a potential drug target. This chapter charts the path from the initial identification of this proteases activity and its validation as a bone fide drug target to the arduous task of the discovery of an inhibitor targeting this protease and finally the path towards the clinic.


Cysteine Protease Trypanosoma Cruzi Target Validation Vinyl Sulfone Sulfone Moiety 
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Copyright information

© Landes Bioscience and Springer Science+Business Media, LLC 2011

Authors and Affiliations

  • Mohammed Sajid
    • 1
  • Stephanie A. Robertson
    • 2
  • Linda S. Brinen
    • 2
    • 3
  • James H. McKerrow
    • 2
  1. 1.Afd. ParasitologieLeiden University Medical CenterLeidenThe Netherlands
  2. 2.Sandler Center for Drug DiscoveryUniversity of California— San FranciscoSan FranciscoUSA
  3. 3.Department of Cellular and Molecular PharmacologyUniversity of California— San FranciscoSan FranciscoUSA

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