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Literature summary for 3.4.13.9 extracted from

  • Mittal, S.; Song, X.; Vig, B.S.; Amidon, G.L.
    Proline prodrug of melphalan targeted to prolidase, a prodrug activating enzyme overexpressed in melanoma (2007), Pharm. Res., 24, 1290-1298.
    View publication on PubMed
Search for more literature for 3.4.13.9

Inhibitors

Inhibitors Comment Organism Structure
N-Benzyloxycarbonyl-L-proline competitive, 60-83% inhibition levels of the enzyme from different cancer cell lines, overview Homo sapiens
N-Benzyloxycarbonyl-L-proline competitive Sus scrofa

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+ required Homo sapiens
Mn2+ required Sus scrofa

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
melphalan + H2O Homo sapiens prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview ?
-
 ?
prophalan-D + H2O Homo sapiens the D-proline prodrug of melphalan, bioactivation and uptake of prolidase-targeted proline prodrugs, prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview ?
-
 ?
prophalan-L + H2O Sus scrofa the L-proline prodrug of melphalan ?
-
 ?
prophalan-L + H2O Homo sapiens the L-proline prodrug of melphalan, bioactivation and uptake of prolidase-targeted proline prodrugs, prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview ?
-
 ?

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
Caco-2 cell
-
 Homo sapiens
-
foreskin
-
 Homo sapiens
-
Hep-G2 cell
-
 Homo sapiens
-
kidney
-
 Sus scrofa
-
MCF-7 cell
-
 Homo sapiens
-
melanoma cell high enzyme expression level Homo sapiens
-
NCI-H522 cell
-
 Homo sapiens
-
SK-MEL-5 cell
-
 Homo sapiens
-
U-251 cell
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 specific activities with melphalan and prodrugs in cancer cell lines, overview Homo sapiens
0.00000059
-
 substrate prophalan-L Sus scrofa

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
melphalan + H2O
-
 Homo sapiens ?
-
 ?
melphalan + H2O prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview Homo sapiens ?
-
 ?
additional information no or poor activity with prophalan-D and melphalan Sus scrofa ?
-
 ?
additional information specific activities with melphalan and prodrugs in cancer cell lines, overview Homo sapiens ?
-
 ?
prophalan-D + H2O
-
 Homo sapiens ?
-
 ?
prophalan-D + H2O the D-proline prodrug of melphalan, bioactivation and uptake of prolidase-targeted proline prodrugs, prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview Homo sapiens ?
-
 ?
prophalan-L + H2O
-
 Homo sapiens ?
-
 ?
prophalan-L + H2O
-
 Sus scrofa ?
-
 ?
prophalan-L + H2O the L-proline prodrug of melphalan Sus scrofa ?
-
 ?
prophalan-L + H2O the L-proline prodrug of melphalan, bioactivation and uptake of prolidase-targeted proline prodrugs, prolidase-dependence of prodrug cytotoxicity in the cell lines compared to that of the parent drug, melphalan, overview Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
prolidase
-
 Homo sapiens
prolidase
-
 Sus scrofa

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
40
-
 assay at Homo sapiens
40
-
 assay at Sus scrofa

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8 8 assay at Homo sapiens
7.8 8 assay at Sus scrofa