Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli strain TX61 | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
A191K | the mutant exhibits about 25% of the catalytic activity of the wild type enzyme. The mutant exhibits nonhyperbolic behavior with respect to dUMP and inhibition of catalysis is reversed by substrate saturation | Homo sapiens |
M190K | the mutant exhibits less than1% of the catalytic activity of the wild type enzyme | Homo sapiens |
R163K | the mutant exhibits an increase in catalytic activity and shows significantly reduced phosphorylation compared to the wild type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
propylene diphosphonate | mixed competitive-noncompetitive inhibitor with respect to dUMP | Homo sapiens | |
ZD1694 | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
phosphoprotein | phosphorylation of the wild type enzyme by casein kinase 2 is selective for the inactive conformation. dUMP inhibits phosphorylation of the wild type enzyme | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
5,10-methylenetetrahydrofolate + dUMP | - |
Homo sapiens | dihydrofolate + dTMP | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000059 | - |
propylene diphosphonate | wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C | Homo sapiens | |
0.0000113 | - |
propylene diphosphonate | mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00144 | - |
wild type enzyme, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C | Homo sapiens | ZD1694 | |
0.034 | - |
mutant enzyme A191K, in 50 mM Tris-HCl, pH 7.4, 1 mM EDTA, 0.2% 2-mercaptoethanol, at 22°C | Homo sapiens | ZD1694 |