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Literature summary for 3.4.21.26 extracted from

  • Van Elzen, R.; Schoenmakers, E.; Brandt, I.; Van Der Veken, P.; Lambeir, A.
    Ligand-induced conformational changes in prolyl oligopeptidase A kinetic approach (2017), Protein Eng. Des. Sel., 30, 219-226 .
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
gene PREP, recombinant expression of N-terminally His6-tagged enzyme in Escherichia coli strain BL21(DE3) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile i.e. KYP-2047, hyperbolic kinetics of KYP-2047 binding to human PREP with pseudo-firstorder rate constant, Van't Hoff plot for binding of KYP-2047 to human PREP, a covalent bond is formed between the nitrile group of KYP-2047 and the active site serine Homo sapiens
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile i.e. KYP-2047 Sus scrofa

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information steady-state kinetics and thermodynamics, comparison of human and porcine enzymes, human and porcine PREP have a similar kinetic behavior, overview Sus scrofa
additional information
-
additional information steady-state kinetics and thermodynamics, comparison of human and porcine enzymes, human and porcine PREP have a similar kinetic behavior, overview Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
bradykinin + H2O Sus scrofa
-
?
-
?
bradykinin + H2O Homo sapiens
-
?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P48147
-
-
Sus scrofa P23687
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His6-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and anion exchange chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
bradykinin + H2O
-
Sus scrofa ?
-
?
bradykinin + H2O
-
Homo sapiens ?
-
?
Gly-Pro-4-nitrophenyl ester + H2O
-
Sus scrofa Gly-Pro + 4-nitrophenol
-
?
Gly-Pro-4-nitrophenyl ester + H2O
-
Homo sapiens Gly-Pro + 4-nitrophenol
-
?
N-benzyloxycarbonyl-Gly-Pro-4-nitrophenyl ester + H2O
-
Sus scrofa N-benzyloxycarbonyl-Gly-Pro + 4-nitrophenol
-
?
N-benzyloxycarbonyl-Gly-Pro-4-nitrophenyl ester + H2O
-
Homo sapiens N-benzyloxycarbonyl-Gly-Pro + 4-nitrophenol
-
?
succinyl-Ala-Pro-4-nitrophenyl ester + H2O
-
Sus scrofa succinyl-Ala-Pro + 4-nitrophenol
-
?
succinyl-Ala-Pro-4-nitrophenyl ester + H2O
-
Homo sapiens succinyl-Ala-Pro + 4-nitrophenol
-
?

Synonyms

Synonyms Comment Organism
PREP
-
Sus scrofa
PREP
-
Homo sapiens
prolyl oligopeptidase
-
Sus scrofa
prolyl oligopeptidase
-
Homo sapiens

Temperature Optimum [┬░C]

Temperature Optimum [┬░C] Temperature Optimum Maximum [┬░C] Comment Organism
37
-
assay at Sus scrofa
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Sus scrofa
7.5 8 recombinant enzyme Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
(2S)-1-[[(2S)-1-(1-oxo-4-phenylbutyl)-2-pyrrolidinyl]carbonyl]-2-pyrrolidinecarbonitrile pH 7.5, 37┬░C, recombinant enzyme Homo sapiens

General Information

General Information Comment Organism
additional information human PREP behaves identically to the porcine homologue, displaying a double bell-shaped pH profile and a pH-dependent solvent kinetic isotope effect of the kcat/Km, features that set it apart from the related exopeptidase dipeptidyl peptidase IV (DPP IV) Sus scrofa
additional information human PREP behaves identically to the porcine homologue, displaying a double bell-shaped pH profile and a pH-dependent solvent kinetic isotope effect of the kcat/Km, features that set it apart from the related exopeptidase dipeptidyl peptidase IV (DPP IV) Homo sapiens