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Literature summary for 3.4.21.26 extracted from

  • Bastos, I.M.; Grellier, P.; Martins, N.F.; Cadavid-Restrepo, G.; de Souza-Ault, M.R.; Augustyns, K.; Teixeira, A.R.; Schrevel, J.; Maigret, B.; da Silveira, J.F.; Santana, J.M.
    Molecular, functional and structural properties of the prolyl oligopeptidase of Trypanosoma cruzi (POP Tc80), which is required for parasite entry into mammalian cells (2005), Biochem. J., 388, 29-38.
    View publication on PubMedView publication on EuropePMC

Activating Compound

Activating Compound Comment Organism Structure
2-mercaptoethanol
-
Trypanosoma cruzi
dithiothreitol up to 14fold stimulation Trypanosoma cruzi

Cloned(Commentary)

Cloned (Comment) Organism
-
Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
phenyl (2S)-2-(((2S)-2-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-1-yl)carbonyl)pyrrolidine-1-carboxylate
-
Trypanosoma cruzi
phenyl (2S)-2-(((2S)-2-(isoxazol-3-ylcarbonyl)pyrrolidin-yl)carbonyl)pyrrolidine-1-carboxylate
-
Trypanosoma cruzi
phenyl (2S)-2-([(2S)-2-[(5-phenylisoxazol-3-yl)carbonyl]pyrrolidin-1-yl]carbonyl)pyrrolidine-1-carboxylate
-
Trypanosoma cruzi
phenyl (2S)-2-[[(2S)-2-([5-[(2E)-3-phenylprop-2-en-1-yl]isoxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate 50% inhibition at 0.01 mM, inhibition of parasite invasion into host cells Trypanosoma cruzi
phenyl (2S)-2-[[(2S)-2-[[5-(trimethylsilyl)isoxazol-3-yl]carbonyl]pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate
-
Trypanosoma cruzi

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.014
-
N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin pH 7.5, native enzyme Trypanosoma cruzi
0.0181
-
N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin pH 7.5, recombinant enzyme Trypanosoma cruzi

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
78320
-
x * 78320, calculated, x * 80000, SDs-PAGE Trypanosoma cruzi
80000
-
x * 78320, calculated, x * 80000, SDs-PAGE Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi Q71MD6
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification no proteolytic modification Trypanosoma cruzi

Reaction

Reaction Comment Organism Reaction ID
Hydrolysis of --Pro-/- and to a lesser extent --Ala-/- in oligopeptides catalytic triad consists of Ser548-Asp631-His667 Trypanosoma cruzi

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information substrates require a proline in position P1, with the exception of N-succinyl-L-Ala-L-Ala-L-Ala-7-amino-4-methylcoumarin Trypanosoma cruzi ?
-
?
N-succinyl-Gly-L-Pro-7-amido-4-methylcoumarin + H2O 24% of the activity with N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin Trypanosoma cruzi ?
-
?
N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin + H2O
-
Trypanosoma cruzi ?
-
?
N-succinyl-L-Ala-L-Ala-L-Ala-7-amido-4-methylcoumarin + H2O 13% of the activity with N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin Trypanosoma cruzi ?
-
?

Subunits

Subunits Comment Organism
? x * 78320, calculated, x * 80000, SDs-PAGE Trypanosoma cruzi
More structural modelling of protein, enzyme is composed of an alpha/beta-hydrolase domain containing a catalytic triad Ser548-Asp631-His667 and a seven-bladed beta-propeller non-catalytic domain Trypanosoma cruzi

Synonyms

Synonyms Comment Organism
POP Tc80
-
Trypanosoma cruzi

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
28.1
-
N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin pH 7.5, native enzyme Trypanosoma cruzi
48.7
-
N-succinyl-Gly-L-Pro-L-Leu-Gly-L-Pro-7-amido-4-methylcoumarin pH 7.5, recombinant enzyme Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000021
-
phenyl (2S)-2-([(2S)-2-[(5-phenylisoxazol-3-yl)carbonyl]pyrrolidin-1-yl]carbonyl)pyrrolidine-1-carboxylate pH 7.5, native enzyme Trypanosoma cruzi
0.00000026
-
phenyl (2S)-2-(((2S)-2-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-1-yl)carbonyl)pyrrolidine-1-carboxylate pH 7.5, native enzyme Trypanosoma cruzi
0.00000028
-
phenyl (2S)-2-[[(2S)-2-([5-[(2E)-3-phenylprop-2-en-1-yl]isoxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate pH 7.5, native enzyme Trypanosoma cruzi
0.00000045
-
phenyl (2S)-2-[[(2S)-2-[[5-(trimethylsilyl)isoxazol-3-yl]carbonyl]pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate pH 7.5, native enzyme Trypanosoma cruzi
0.00000048
-
phenyl (2S)-2-([(2S)-2-[(5-phenylisoxazol-3-yl)carbonyl]pyrrolidin-1-yl]carbonyl)pyrrolidine-1-carboxylate pH 7.5, recombinant enzyme Trypanosoma cruzi
0.0000008
-
phenyl (2S)-2-[[(2S)-2-([5-[(2E)-3-phenylprop-2-en-1-yl]isoxazol-3-yl]carbonyl)pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate pH 7.5, recombinant enzyme Trypanosoma cruzi
0.0000009
-
phenyl (2S)-2-(((2S)-2-(1,3-thiazol-2-ylcarbonyl)pyrrolidin-1-yl)carbonyl)pyrrolidine-1-carboxylate pH 7.5, recombinant enzyme Trypanosoma cruzi
0.0000015
-
phenyl (2S)-2-[[(2S)-2-[[5-(trimethylsilyl)isoxazol-3-yl]carbonyl]pyrrolidin-1-yl]carbonyl]pyrrolidine-1-carboxylate pH 7.5, recombinant enzyme Trypanosoma cruzi
0.000072
-
phenyl (2S)-2-(((2S)-2-(isoxazol-3-ylcarbonyl)pyrrolidin-yl)carbonyl)pyrrolidine-1-carboxylate pH 7.5, native enzyme Trypanosoma cruzi
0.000083
-
phenyl (2S)-2-(((2S)-2-(isoxazol-3-ylcarbonyl)pyrrolidin-yl)carbonyl)pyrrolidine-1-carboxylate pH 7.5, recombinant enzyme Trypanosoma cruzi