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Literature summary for 3.4.21.26 extracted from

  • Szeltner, Z.; Juhasz, T.; Szamosi, I.; Rea, D.; Fueloep, V.; Modos, K.; Juliano, L.; Polgar, L.
    The loops facing the active site of prolyl oligopeptidase are crucial components in substrate gating and specificity (2013), Biochim. Biophys. Acta, 1834, 98-111.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
T202C the mutation increases the flexibility of loop A, enhancing the catalytic efficiency 2fold beyond that of the native enzyme Homo sapiens
T202C/T590C the mutant shows more than 10fold increased Km and increased kcat values towards Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala at pH 8.0 compared to the wild type enzyme Homo sapiens
T590C variant displays an altered substrate preference profile, with reduced ligand binding capacity. The mutation in loop B increased the preference for shorter peptides, indicating a role in substrate gating Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
KYP-2047 i.e. 4-phenylbutanoyl-l-prolyl-2(S)-cyanopyrrolidine, highly potent covalent reversible competitive inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00081
-
Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala wild type enzyme, at pH 8.0 and 25┬░C Homo sapiens
0.00921
-
Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala mutant enzyme T202C/T590C, at pH 8.0 and 25┬░C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-Glu-Gly-L-Phe-Gly-L-Pro-L-Phe-Gly-L-4-nitrophenylalanine-L-Ala + H2O
-
Homo sapiens 2-aminobenzoyl-Glu-Gly-L-Phe-Gly-L-Pro + L-Phe-Gly-L-4-nitrophenylalanine-L-Ala
-
?
2-aminobenzoyl-Gly-L-Phe-Gly-L-Pro-L-Phe-Gly-L-4-nitrophenylalanine-L-Ala + H2O
-
Homo sapiens 2-aminobenzoyl-Gly-L-Phe-Gly-L-Pro + L-Phe-Gly-L-4-nitrophenylalanine-L-Ala
-
?
2-aminobenzoyl-Gly-L-Phe-L-Arg-L-Pro-L-4-nitrophenylalanine-L-Arg-L-Ala + H2O
-
Homo sapiens 2-aminobenzoyl-Gly-L-Phe-L-Arg-L-Pro + L-4-nitrophenylalanine-L-Arg-L-Ala
-
?
2-aminobenzoyl-L-Ser-L-Pro-L-4-nitrophenylalanine-L-Ala + H2O
-
Homo sapiens 2-aminobenzoyl-L-Ser-L-Pro + 4-nitrophenylalanine-L-Ala
-
?
Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala + H2O
-
Homo sapiens Abz-Gly-L-Phe-L-Arg-L-Pro + L-Phe(NO2)-L-Arg-L-Ala
-
?
Abz-Gly-L-Phe-L-Ser-L-Pro-L-Phe-L-Arg-L-Ser-L-Ser-L-Arg-L-Ile-Gly-L-Glu-L-Ile-L-Lys-L-Glu-L-Glu-L-Gln-N-(2,4-dinitrophenyl)-ethylenediamine + H2O
-
Homo sapiens Abz-Gly-L-Phe-L-Ser-L-Pro + L-Phe-L-Arg-L-Ser-L-Ser-L-Arg-L-Ile-Gly-L-Glu-L-Ile-L-Lys-L-Glu-L-Glu-L-Gln-N-(2,4-dinitrophenyl)-ethylenediamine
-
?
Z-Gly-Pro-2-naphthylamide + H2O
-
Homo sapiens Z-Gly-Pro + 2-naphthylamine
-
?

Synonyms

Synonyms Comment Organism
PEP
-
Homo sapiens
POP
-
Homo sapiens
PREP
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.97
-
Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala wild type enzyme, at pH 8.0 and 25┬░C Homo sapiens
1.31
-
Abz-Gly-L-Phe-L-Arg-L-Pro-L-Phe(NO2)-L-Arg-L-Ala mutant enzyme T202C/T590C, at pH 8.0 and 25┬░C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000015
-
wild type enzyme, at pH 8.0 and 25┬░C Homo sapiens KYP-2047