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Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor
(Informa HealthcareLondon, 2013-08)
Cruzain is the major cysteine protease of Trypanosoma cruzi, the infectious agent responsible for Chagas disease, and cruzain inhibitors display considerable antitrypanosomal activity. In the present work we elucidated ...
Pharmacophore Model of Cruzain Inhibitors
(WILEY-V C H VERLAG GMBH, 2009)
Chagas disease, caused by the protozoan Trypanosoma cruzi, is one of the most serious amongst the so-called neglected diseases in Latin America, specially in Brazil. So far there has been no effective treatment for the ...
Molecular features for antitrypanosomal activity of thiosemicarbazones revealed by OPS-PLS QSAR studies
(Bentham ScienceBussum, 2012-11)
A quantitative structure-activity relationship analysis was employed to explore the relationship between the molecular structure of thiosemicarbazone analogues and the inhibition of the cysteine protease cruzain, a validated ...
Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents
(PERGAMON-ELSEVIER SCIENCE LTD, 2010)
In previous studies, we identified promising anti-Trypanosoma cruzi cruzain inhibitors based on thiazolylhydrazones. To optimize this series, a number of medicinal chemistry directions were explored and new thiazolylhydrazones ...
Dissecting a novel allosteric mechanism of cruzain: A computer-aided approach
(Public Library Science, 2019-01-25)
Trypanosoma cruzi is the causative agent of Chagas disease, a neglected infection affecting millions of people in tropical regions. There are several chemotherapeutic agents for the treatment of this disease, but most of ...
Comparison of the specificity, stability and individual rate constants with respective activation parameters for the peptidase activity of cruzipain and its recombinant form, cruzain, from Trypanosoma cruzi
(Blackwell Publishing Ltd, 2001-12-01)
The Trypanosoma cruzi cysteine protease cruzipain contains a 130-amino-acid C-terminal extension, in addition to the catalytic domain. Natural cruzipain is a complex of isoforms, because of the simultaneous expression of ...