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Literature summary for 3.4.22.51 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
Search for more literature for 3.4.22.51

Inhibitors

Inhibitors Comment Organism Structure
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
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
additional information AM1 semi-empirical molecular modeling studies analysing cruzain inhibitory activity, overview Trypanosoma cruzi
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

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

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

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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