Cruzain : the path from target validation to the clinic

Adv Exp Med Biol. 2011;712:100-15. doi: 10.1007/978-1-4419-8414-2_7.


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.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Chagas Disease / drug therapy
  • Chagas Disease / parasitology
  • Cysteine Endopeptidases / chemistry
  • Cysteine Endopeptidases / metabolism*
  • Cysteine Proteinase Inhibitors / pharmacology
  • Dipeptides / chemistry
  • Dipeptides / pharmacology
  • Dipeptides / therapeutic use
  • Humans
  • Molecular Sequence Data
  • Protozoan Proteins / antagonists & inhibitors
  • Protozoan Proteins / chemistry
  • Protozoan Proteins / metabolism*
  • Reproducibility of Results
  • Translational Medical Research*
  • Vinyl Compounds / chemistry
  • Vinyl Compounds / pharmacology
  • Vinyl Compounds / therapeutic use


  • Cysteine Proteinase Inhibitors
  • Dipeptides
  • N-pip-phenylalanine-homophenylalanine-vinyl sulfone phenyl
  • Protozoan Proteins
  • Vinyl Compounds
  • Cysteine Endopeptidases
  • cruzain, Trypanosoma cruzi