Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.5.1.2 extracted from

  • Forlani, G.; Sabbioni, G.; Ragno, D.; Petrollino, D.; Borgatti, M.
    Phenyl-substituted aminomethylene-bisphosphonates inhibit human P5C reductase and show antiproliferative activity against proline-hyperproducing tumour cells (2021), J. Enzyme Inhib. Med. Chem., 36, 1248-1257 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.5.1.2

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
([[(3,5-dibromophenyl)methyl]amino]methylene)bis(phosphonic acid) competitive inhibition against both 1-pyrroline 5-carboxylate and NADPH. Growth of myelogenous erythroleukemic K562 and epithelial breast cancer MDA-MB-231 cell lines is progressively impaired by concentrations ranging from 1-100 microM Homo sapiens
([[(3,5-dichlorophenyl)methyl]amino]methylene)bis(phosphonic acid) competitive inhibition against both 1-pyrroline 5-carboxylate and NADPH Homo sapiens
4-bromopargyline
-
 Homo sapiens
Pargyline
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.088
-
 NADH pH 7.5, 30°C Homo sapiens
0.223
-
 NADPH pH 7.5, 30°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P32322
-
-

Source Tissue

Source Tissue Comment Organism Textmining
K-562 cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-pyrroline-5-carboxylate + NADH + H+
-
 Homo sapiens L-proline + NAD+
-
 ?
1-pyrroline-5-carboxylate + NADPH + H+
-
 Homo sapiens L-proline + NADP+
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00039
-
 substrate NADPH, pH 7.5, 30°C Homo sapiens ([[(3,5-dibromophenyl)methyl]amino]methylene)bis(phosphonic acid)
0.00048
-
 substrate NADH, pH 7.5, 30°C Homo sapiens ([[(3,5-dibromophenyl)methyl]amino]methylene)bis(phosphonic acid)
0.00074
-
 substrate NADPH, pH 7.5, 30°C Homo sapiens ([[(3,5-dichlorophenyl)methyl]amino]methylene)bis(phosphonic acid)
0.00078
-
 substrate NADH, pH 7.5, 30°C Homo sapiens ([[(3,5-dichlorophenyl)methyl]amino]methylene)bis(phosphonic acid)
0.0087
-
 substrate NADPH, pH 7.5, 30°C Homo sapiens 4-bromopargyline
0.081
-
 substrate NADPH, pH 7.5, 30°C Homo sapiens Pargyline
0.234
-
 substrate NADH, pH 7.5, 30°C Homo sapiens 4-bromopargyline
10
-
 IC50 value above 10 mM, substrate NADH, pH 7.5, 30°C Homo sapiens Pargyline