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Literature summary extracted from

  • Alves, L.C.; Melo, R.L.; Cezari, M.H.S.; Sanderson, S.J.; Mottram, J.C.; Coombs, G.H.; Juliano, L.; Juliano, M.A.
    Analysis of the S2 subsite specificities of the recombinant cysteine proteinases CPB of Leishmania mexicana, and cruzain of Trypanosoma cruzi, using fluorescent substrates containing non-natural basic amino acids (2001), Mol. Biochem. Parasitol., 117, 137-143.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.B5 benzoyl-(4-aminomethyl-cyclohexyl-alanine)-R-4-methylcoumarin-7-amide
-
 Leishmania mexicana

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.22.B5 0.0014
-
 benzoyl-FR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.0038
-
 benzoyl-(4-aminomethyl-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.0114
-
 benzoyl-(3-pyridylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.012
-
 benzoyl-RR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.021
-
 benzoyl-(4-aminomethyl-N-isopropyl-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.035
-
 benzoyl-(4-guanidine-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.051
-
 benzoyl-HR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.51 0.0011
-
 benzyloxycarbonyl-FR-aminomethyl coumarin pH 6.3, 37°C Trypanosoma cruzi
3.4.22.51 0.0012
-
 benzoyl-Phe-Arg-7-amido-4-methylcoumarin pH 6.3, 37°C Trypanosoma cruzi
3.4.22.51 0.0119
-
 benzoyl-RR-aminomethyl coumarin pH 6.3, 37°C Trypanosoma cruzi
3.4.22.51 0.043
-
 benzoyl-His-Arg-7-amido-4-methylcoumarin pH 6.3, 37°C Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.B5 Leishmania mexicana
-
-
-
3.4.22.51 Trypanosoma cruzi Q598P5
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.B5 benzoyl-(3-pyridylalanine)-R-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-(3-pyridylalanine)-R + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-(4-aminomethyl-N-isopropyl-phenylalanine)-R-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-(4-aminomethyl-N-isopropyl-phenylalanine) + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-(4-aminomethyl-phenylalanine)-R-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-(4-aminomethyl-phenylalanine)-R + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-(4-guanidine-phenylalanine)-R-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-(4-guanidine-phenylalanine)-R + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-FR-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-FR + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-HR-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-HR + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 benzoyl-RR-4-methylcoumarin-7-amide + H2O
-
 Leishmania mexicana benzoyl-RR + 7-amino-4-methylcoumarin
-
 ?
3.4.22.B5 additional information no hydrolysis of benzoyl-(4-piperidinylalanine)-R-4-methylcoumarin-7-amide and benzoyl-(4-aminocyclohexylalanine)-R-4-methylcoumarin-7-amide Leishmania mexicana ?
-
 ?
3.4.22.51 benzoyl-FR-4-methylcoumarin 7-amide + H2O fluorigenic substrates based on this peptide, substitution of Phe results in less susceptible substrates Trypanosoma cruzi ?
-
 ?
3.4.22.51 benzoyl-His-Arg-7-amido-4-methylcoumarin + H2O
-
 Trypanosoma cruzi benzoyl-His-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.22.51 benzoyl-HR-4-methylcoumarin 7-amide + H2O less susceptible substrate Trypanosoma cruzi ?
-
 ?
3.4.22.51 benzoyl-Phe-Arg-4-methylcoumarin-7-amide + H2O fluorogenic substrates based on the peptide benzoyl-Phe-Arg-4-methylcoumarin-7-amide Trypanosoma cruzi ?
-
 ?
3.4.22.51 benzoyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Trypanosoma cruzi benzoyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.22.51 benzoyl-RR-4-methylcoumarin 7-amide + H2O less susceptible substrate Trypanosoma cruzi ?
-
 ?
3.4.22.51 benzyloxycarbonyl-Phe-Arg-4-methylcoumarin 7-amide + H2O
-
 Trypanosoma cruzi ?
-
 ?

Temperature Optimum [°C]

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.22.B5 0.18
-
 benzoyl-(4-aminomethyl-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.2
-
 benzoyl-RR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 0.3
-
 benzoyl-HR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 1.1
-
 benzoyl-(4-guanidine-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 1.4
-
 benzoyl-(4-aminomethyl-N-isopropyl-phenylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 1.45
-
 benzoyl-(3-pyridylalanine)-R-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.B5 3.9
-
 benzoyl-FR-4-methylcoumarin-7-amide pH 6.3, 37°C Leishmania mexicana
3.4.22.51 0.0783
-
 benzoyl-RR-aminomethyl coumarin
-
 Trypanosoma cruzi
3.4.22.51 0.158
-
 benzyloxycarbonyl-FR-aminomethyl coumarin
-
 Trypanosoma cruzi
3.4.22.51 0.172
-
 benzoyl-His-Arg-7-amido-4-methylcoumarin
-
 Trypanosoma cruzi
3.4.22.51 0.193
-
 benzoyl-Phe-Arg-7-amido-4-methylcoumarin
-
 Trypanosoma cruzi