Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli BL21(DE3) cells | Plasmodium falciparum |
Protein Variants | Comment | Organism |
---|---|---|
F46A | the mutation does not affect the nucleotide hydrolase activity of dUTPase | Plasmodium falciparum |
I117A | the mutation does not affect the nucleotide hydrolase activity of dUTPase | Plasmodium falciparum |
K96A | the mutation does not affect the nucleotide hydrolase activity of dUTPase | Plasmodium falciparum |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione | - |
Plasmodium falciparum | |
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine | - |
Plasmodium falciparum | |
2',5'-dideoxy-5'-(tritylamino)uridine | - |
Plasmodium falciparum |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0016 | - |
dUTP | wild type enzyme, at pH 8.0 and 25°C | Plasmodium falciparum | |
0.0017 | - |
dUTP | mutant enzyme I117A, at pH 8.0 and 25°C | Plasmodium falciparum | |
0.0018 | - |
dUTP | mutant enzyme F46A, at pH 8.0 and 25°C | Plasmodium falciparum | |
0.0019 | - |
dUTP | mutant enzyme K96A, at pH 8.0 and 25°C | Plasmodium falciparum |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Plasmodium falciparum | Q8II92 | - |
- |
Purification (Comment) | Organism |
---|---|
phosphocellulose column chromatography | Plasmodium falciparum |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
dUTP + H2O | - |
Plasmodium falciparum | dUMP + diphosphate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
deoxyuridine 5-triphosphate nucleotidohydrolase | - |
Plasmodium falciparum |
dUTPase | - |
Plasmodium falciparum |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
11.33 | - |
dUTP | mutant enzyme F46A, at pH 8.0 and 25°C | Plasmodium falciparum | |
11.67 | - |
dUTP | mutant enzyme K96A, at pH 8.0 and 25°C | Plasmodium falciparum | |
11.67 | - |
dUTP | wild type enzyme, at pH 8.0 and 25°C | Plasmodium falciparum | |
12 | - |
dUTP | mutant enzyme I117A, at pH 8.0 and 25°C | Plasmodium falciparum |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00004 | - |
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00004 | - |
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00009 | - |
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00011 | - |
2',5'-dideoxy-5'-(tritylamino)uridine | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00015 | - |
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0002 | - |
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0002 | - |
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00021 | - |
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00024 | - |
2',5'-dideoxy-5'-(tritylamino)uridine | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00027 | - |
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.00039 | - |
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0006 | - |
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0006 | - |
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0007 | - |
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0008 | - |
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0008 | - |
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0012 | - |
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0013 | - |
2',5'-dideoxy-5'-(tritylamino)uridine | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0016 | - |
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0018 | - |
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0019 | - |
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0044 | - |
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0048 | - |
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine | mutant enzyme K96A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.005 | - |
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine | wild type enzyme, at pH 8.0 and 25° | Plasmodium falciparum | |
0.006 | - |
1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.008 | - |
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.013 | - |
1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.017 | - |
1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.02 | - |
2',5'-dideoxy-5'-(tritylamino)uridine | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.0203 | - |
1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.028 | - |
1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.029 | - |
1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.035 | - |
1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.225 | - |
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine | mutant enzyme F46A, at pH 8.0 and 25° | Plasmodium falciparum | |
0.406 | - |
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine | mutant enzyme I117A, at pH 8.0 and 25° | Plasmodium falciparum |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
6100 | - |
dUTP | mutant enzyme K96A, at pH 8.0 and 25°C | Plasmodium falciparum | |
6300 | - |
dUTP | mutant enzyme F46A, at pH 8.0 and 25°C | Plasmodium falciparum | |
7100 | - |
dUTP | mutant enzyme I117A, at pH 8.0 and 25°C | Plasmodium falciparum | |
7300 | - |
dUTP | wild type enzyme, at pH 8.0 and 25°C | Plasmodium falciparum |