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Literature summary 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

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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.14.2 Diprotin A not selective for the enzyme Homo sapiens
3.4.14.2 Ile cyanothiazolidide not selective for the enzyme Homo sapiens
3.4.14.2 Lys piperidide not selective for the enzyme Homo sapiens
3.4.14.2 Lys thiazolidide not selective for the enzyme Homo sapiens
3.4.14.2 threo-Ile thiazolidide not selective for the enzyme Homo sapiens
3.4.14.2 Val pyrrolidide not selective for the enzyme Homo sapiens
3.4.14.2 Val thiazolidide not selective for the enzyme Homo sapiens
3.4.14.5 cyclohexylglycine thiazolidide
-
 Homo sapiens
3.4.14.5 Diprotin A
-
 Homo sapiens
3.4.14.5 Ile cyanothiazolidide
-
 Homo sapiens
3.4.14.5 Lys piperidide
-
 Homo sapiens
3.4.14.5 Lys thiazolidide
-
 Homo sapiens
3.4.14.5 threo-Ile thiazolidide
-
 Homo sapiens
3.4.14.5 Val pyrrolidide
-
 Homo sapiens
3.4.14.5 Val thiazolidide
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.14.2 0.003
-
 Nle-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.2 0.003
-
 Nle-Pro-rhodamine pH 7.5, 37°C Homo sapiens
3.4.14.2 0.006
-
 Nle-Nle-rhodamine pH 7.5, 37°C Homo sapiens
3.4.14.2 0.011
-
 Lys-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.2 0.032
-
 Ala-Pro-amino-4-trifluoromethylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.2 0.149
-
 Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.2 0.215
-
 Lys-Ala-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.5 0.022
-
 Ala-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.5 0.034
-
 norleucine-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.5 0.035
-
 Lys-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens
3.4.14.5 0.035
-
 norleucine-Pro-rhodamine pH 7.5, 37°C Homo sapiens
3.4.14.5 0.063
-
 Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 37°C Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.14.2 lysosomal
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.4.14.2 Homo sapiens Q9UHL4
-
-
3.4.14.5 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.14.2 from placenta Homo sapiens
3.4.14.5 recombinant enzyme from insect cells, rapidly to homogeneity Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.14.2 placenta
-
 Homo sapiens
-
3.4.14.5 kidney
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.14.2 Ala-Pro-amino-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens Ala-Pro + amino-4-trifluoromethylcoumarin
-
 ?
3.4.14.2 Gly-Ala-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-Ala + 7-amino-4-methylcoumarin
-
 ?
3.4.14.2 Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.2 Lys-Ala-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Lys-Ala + 7-amino-4-methylcoumarin
-
 ?
3.4.14.2 Lys-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Lys-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.2 additional information specific for Pro at position P1 Homo sapiens ?
-
 ?
3.4.14.2 Nle-Nle-rhodamine + H2O
-
 Homo sapiens Nle-Nle + rhodamine
-
 ?
3.4.14.2 Nle-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Nle-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.2 Nle-Pro-rhodamine + H2O
-
 Homo sapiens Nle-Pro + rhodamine
-
 ?
3.4.14.5 Ala-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Ala-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.5 Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.5 Lys-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Lys-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.5 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 ?
-
 ?
3.4.14.5 additional information enzyme is involved in glucose metabolism in contributing to the regulation of glucagon family peptides Homo sapiens ?
-
 ?
3.4.14.5 norleucine-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens norleucine-Pro + 7-amino-4-methylcoumarin
-
 ?
3.4.14.5 norleucine-Pro-rhodamine + H2O
-
 Homo sapiens norleucine-Pro + rhodamine
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.14.2 dipeptidyl peptidase
-
 Homo sapiens
3.4.14.2 DPP-II
-
 Homo sapiens
3.4.14.2 More enzyme belongs to the Pro-X carboxypeptidase family S28 Homo sapiens
3.4.14.5 dipeptidyl peptidase IV
-
 Homo sapiens
3.4.14.5 DPP-IV
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.14.2 37
-
 assay at Homo sapiens
3.4.14.5 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.14.2 5.5 6
-
 Homo sapiens
3.4.14.5 8 8.5
-
 Homo sapiens

pH Range

EC Number pH Minimum pH Maximum Comment Organism
3.4.14.2 3.5 8.5
-
 Homo sapiens
3.4.14.5 additional information
-
 the enzyme is essentially inactive at acidic pH Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.14.2 0.00017
-
 Lys thiazolidide pH 7.5, 37°C Homo sapiens
3.4.14.2 0.00056
-
 Ile cyanothiazolidide pH 7.5, 37°C Homo sapiens
3.4.14.2 0.00065
-
 Lys piperidide pH 7.5, 37°C Homo sapiens
3.4.14.2 0.0097
-
 threo-Ile thiazolidide pH 7.5, 37°C Homo sapiens
3.4.14.2 0.0153
-
 Val thiazolidide pH 7.5, 37°C Homo sapiens
3.4.14.2 0.0408
-
 Diprotin A pH 7.5, 37°C Homo sapiens
3.4.14.2 0.1
-
 Val pyrrolidide above, pH 7.5, 37°C Homo sapiens
3.4.14.5 0.000001
-
 Ile cyanothiazolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.000044
-
 cyclohexylglycine thiazolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.0002
-
 Lys thiazolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.00022
-
 threo-Ile thiazolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.00028
-
 Val thiazolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.00067
-
 Lys piperidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.00089
-
 Val pyrrolidide pH 7.5, 37° Homo sapiens
3.4.14.5 0.0035
-
 Diprotin A pH 7.5, 37° Homo sapiens