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Literature summary 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

Cloned(Commentary)

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

Protein Variants

EC Number Protein Variants Comment Organism
3.6.1.23 F46A the mutation does not affect the nucleotide hydrolase activity of dUTPase Plasmodium falciparum
3.6.1.23 I117A the mutation does not affect the nucleotide hydrolase activity of dUTPase Plasmodium falciparum
3.6.1.23 K96A the mutation does not affect the nucleotide hydrolase activity of dUTPase Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.1.23 1-[(2E)-4-(trityloxy)but-2-en-1-yl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[(2R,5S)-5-([[tert-butyl(diphenyl)silyl]oxy]methyl)-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[(2R,5S)-5-[(trityloxy)methyl]-2,5-dihydrofuran-2-yl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[4-hydroxy-3-[(tritylamino)methyl]butyl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione
-
 Plasmodium falciparum
3.6.1.23 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine
-
 Plasmodium falciparum
3.6.1.23 2',5'-dideoxy-5'-(tritylamino)uridine
-
 Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.6.1.23 0.0016
-
 dUTP wild type enzyme, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 0.0017
-
 dUTP mutant enzyme I117A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 0.0018
-
 dUTP mutant enzyme F46A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 0.0019
-
 dUTP mutant enzyme K96A, at pH 8.0 and 25°C Plasmodium falciparum

Organism

EC Number Organism UniProt Comment Textmining
3.6.1.23 Plasmodium falciparum Q8II92
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.6.1.23 phosphocellulose column chromatography Plasmodium falciparum

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.6.1.23 11.33
-
 dUTP mutant enzyme F46A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 11.67
-
 dUTP mutant enzyme K96A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 11.67
-
 dUTP wild type enzyme, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 12
-
 dUTP mutant enzyme I117A, at pH 8.0 and 25°C Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.6.1.23 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
3.6.1.23 0.00004
-
 1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme K96A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.00011
-
 2',5'-dideoxy-5'-(tritylamino)uridine mutant enzyme K96A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 0.00015
-
 1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme K96A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.0002
-
 1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione wild type enzyme, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.00024
-
 2',5'-dideoxy-5'-(tritylamino)uridine wild type enzyme, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 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
3.6.1.23 0.0006
-
 1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme I117A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.0007
-
 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione wild type enzyme, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 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
3.6.1.23 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
3.6.1.23 0.0013
-
 2',5'-dideoxy-5'-(tritylamino)uridine mutant enzyme I117A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.0018
-
 1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione wild type enzyme, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.0044
-
 1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme I117A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 0.0048
-
 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine mutant enzyme K96A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 0.005
-
 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine wild type enzyme, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.008
-
 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme I117A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 0.013
-
 1-[[2-(trityloxy)ethoxy]methyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme F46A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.02
-
 2',5'-dideoxy-5'-(tritylamino)uridine mutant enzyme F46A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.028
-
 1-[3-(tritylamino)propyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme F46A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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
3.6.1.23 0.035
-
 1-[6-(tritylamino)hexyl]pyrimidine-2,4(1H,3H)-dione mutant enzyme F46A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 0.225
-
 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine mutant enzyme F46A, at pH 8.0 and 25° Plasmodium falciparum
3.6.1.23 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]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.6.1.23 6100
-
 dUTP mutant enzyme K96A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 6300
-
 dUTP mutant enzyme F46A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 7100
-
 dUTP mutant enzyme I117A, at pH 8.0 and 25°C Plasmodium falciparum
3.6.1.23 7300
-
 dUTP wild type enzyme, at pH 8.0 and 25°C Plasmodium falciparum