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Literature summary for 3.6.1.23 extracted from

  • Recio, E.; Musso-Buendia, A.; Vidal, A.E.; Ruda, G.F.; Kasinathan, G.; Nguyen, C.; Ruiz-Perez, L.M.; Gilbert, I.H.; Gonzalez-Pacanowska, D.
    Site-directed mutagenesis provides insights into the selective binding of trityl derivatives to Plasmodium falciparum dUTPase (2011), Eur. J. Med. Chem., 46, 3309-3314.
    View publication on PubMed
Search for more literature for 3.6.1.23

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Plasmodium falciparum

Protein Variants

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

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 [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

Organism UniProt Comment Textmining
Plasmodium falciparum Q8II92
-
-

Purification (Commentary)

Purification (Comment) Organism
phosphocellulose column chromatography Plasmodium falciparum

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dUTP + H2O
-
 Plasmodium falciparum dUMP + diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
deoxyuridine 5’-triphosphate nucleotidohydrolase
-
 Plasmodium falciparum
dUTPase
-
 Plasmodium falciparum

Turnover Number [1/s]

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 [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 [mM/s]

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