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Literature summary extracted from

  • Trossini, G.; Malvezzi, A.; Amaral, A.; Rangel-Yagui, C.; Izidoro, M.; Cezari, M.; Juliano, L.; Chin, C.; Menezes, C.; Ferreira, E.
    Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: Investigation of a new target in Trypanosoma cruzi (2010), J. Enzyme Inhib. Med. Chem., 25, 62-67.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.51 benznidazole presents 80% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.01 mM Trypanosoma cruzi
3.4.22.51 hydroxymethylnitrofurazone presents 100% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to complete inhibition in trypomastigotes at 0.005 mM Trypanosoma cruzi
3.4.22.51 additional information AM1 semi-empirical molecular modeling studies analysing cruzain inhibitory activity, overview Trypanosoma cruzi
3.4.22.51 nitrofurazone a 5-nitro-2-furfurylidenesemicarbazone, presents 90% inhibitory activity against amastigotes in LLC-MK2 cell culture infected with amastigote and trypomastigote forms of the parasite, leads to parasite recrudescence in trypomastigotes on the 15th day at 0.005 mM Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.51 Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.51 Bz-Phe-Arg-4-methylcoumaryl-7-amide + H2O
-
 Trypanosoma cruzi Bz-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.22.51 37
-
 assay at Trypanosoma cruzi

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.22.51 6.5
-
 assay at Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.51 0.0106
-
 pH 6.5, 37°C Trypanosoma cruzi hydroxymethylnitrofurazone
3.4.22.51 0.0228
-
 pH 6.5, 37°C Trypanosoma cruzi nitrofurazone