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Literature summary for 3.4.14.5 extracted from

  • Leiting, B.; Pryor, K.D.; Wu, J.K.; Marsilio, F.; Patel, R.A.; Craik, C.S.; Ellman, J.A.; Cummings, R.T.; Thornberry, N.A.
    Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII (2003), Biochem. J., 371, 525-532.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine enzyme is a potential target for treatment of metabolic diseases Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression in insect cells via baculovirus infection as secreted soluble enzyme with Asp29 to the end without any fusion tag Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclohexylglycine thiazolidide
-
Homo sapiens
Diprotin A
-
Homo sapiens
Ile cyanothiazolidide
-
Homo sapiens
Lys piperidide
-
Homo sapiens
Lys thiazolidide
-
Homo sapiens
threo-Ile thiazolidide
-
Homo sapiens
Val pyrrolidide
-
Homo sapiens
Val thiazolidide
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.022
-
Ala-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
0.034
-
norleucine-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
0.035
-
Lys-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
0.035
-
norleucine-Pro-rhodamine pH 7.5, 37°C Homo sapiens
0.063
-
Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme is involved in glucose metabolism in contributing to the regulation of glucagon family peptides ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme from insect cells, rapidly to homogeneity Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ala-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Ala-Pro + 7-amino-4-methylcoumarin
-
?
Gly-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
?
Lys-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Lys-Pro + 7-amino-4-methylcoumarin
-
?
additional information substrate specificity, positional scanning combinatorial dipeptide library profile shows that the enzyme is specific for Pro at P1 position and accepts a broad amino acid spectrum at P2 position with isoleucine and norleucine resulting in highest activity, norleucine-norleucine-rhodamine is no substrate, Gly-Ala-7-amido-4-methylcoumarin and Lys-Ala-7-amido-4-methylcoumarin are poor substrates Homo sapiens ?
-
?
additional information enzyme is involved in glucose metabolism in contributing to the regulation of glucagon family peptides Homo sapiens ?
-
?
norleucine-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens norleucine-Pro + 7-amino-4-methylcoumarin
-
?
norleucine-Pro-rhodamine + H2O
-
Homo sapiens norleucine-Pro + rhodamine
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
DPP-IV
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8 8.5
-
Homo sapiens

pH Range

pH Minimum pH Maximum Comment Organism
additional information
-
the enzyme is essentially inactive at acidic pH Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
Ile cyanothiazolidide pH 7.5, 37° Homo sapiens
0.000044
-
cyclohexylglycine thiazolidide pH 7.5, 37° Homo sapiens
0.0002
-
Lys thiazolidide pH 7.5, 37° Homo sapiens
0.00022
-
threo-Ile thiazolidide pH 7.5, 37° Homo sapiens
0.00028
-
Val thiazolidide pH 7.5, 37° Homo sapiens
0.00067
-
Lys piperidide pH 7.5, 37° Homo sapiens
0.00089
-
Val pyrrolidide pH 7.5, 37° Homo sapiens
0.0035
-
Diprotin A pH 7.5, 37° Homo sapiens