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Literature summary for 3.6.1.23 extracted from

  • Baragana, B.; McCarthy, O.; Sanchez, P.; Bosch-Navarrete, C.; Kaiser, M.; Brun, R.; Whittingham, J.L.; Roberts, S.M.; Zhou, X.X.; Wilson, K.S.; Johansson, N.G.; Gonzalez-Pacanowska, D.; Gilbert, I.H.
    beta-Branched acyclic nucleoside analogues as inhibitors of Plasmodium falciparum dUTPase (2011), Bioorg. Med. Chem., 19, 2378-2391.
    View publication on PubMed

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
1-(2-amido-4-trityloxybutyl)uracil
-
Plasmodium falciparum
1-(2-dimethylamido-4-trityloxybutyl)uracil
-
Plasmodium falciparum
1-(2-morpholinamido-4-trityloxybutyl)uracil
-
Plasmodium falciparum
1-[2-(acetamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
Plasmodium falciparum
1-[2-(acetamido)-4-(triphenylmethyl)aminobutyl]uracil
-
Plasmodium falciparum
1-[2-(carbobenzoxymethyl)-4-(triphenylmethyl)aminobutyl]uracil
-
Plasmodium falciparum
1-[2-(carboethoxyethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(carboxy)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
Plasmodium falciparum
1-[2-(carboxy)-4-(triphenylmethyl)aminobutyl]uracil
-
Plasmodium falciparum
1-[2-(carboxyethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(diethylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
Plasmodium falciparum
1-[2-(ethylamido)-4-(tert-butyldiphenylsilyloxy) butyl]uracil
-
Plasmodium falciparum
1-[2-(hydroxyethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(methoxyethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(methylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
Plasmodium falciparum
1-[2-(N,N-dimethylaminoethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(N-benzyloxycarbonylpiperazinamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil
-
Plasmodium falciparum
1-[2-(N-methylpiperazine)amido-4-trityloxybutyl]uracil
-
Plasmodium falciparum
1-[2-(tert-butyldiphenylsilyloxyethylamido)-4-trityloxybutyl]uracil
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum Q8II92
-
-

Purification (Commentary)

Purification (Comment) Organism
phosphocellulose column chromatography and Superdex 200 gel filtration 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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
1-[2-(carboxyethylamido)-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0004
-
1-[2-(hydroxyethylamido)-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0005
-
1-[2-(carboethoxyethylamido)-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0013
-
1-(2-amido-4-trityloxybutyl)uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0014
-
1-[2-(methoxyethylamido)-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0016
-
1-[2-(carboxy)-4-(tert-butyldiphenylsilyloxy)butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0021
-
1-(2-morpholinamido-4-trityloxybutyl)uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0027
-
1-(2-dimethylamido-4-trityloxybutyl)uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0036
-
1-[2-(methylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.005
-
1-[2-(acetamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0055
-
1-[2-(acetamido)-4-(triphenylmethyl)aminobutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0056
-
1-[2-(N-methylpiperazine)amido-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0057
-
1-[2-(ethylamido)-4-(tert-butyldiphenylsilyloxy) butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0065
-
1-[2-(carbobenzoxymethyl)-4-(triphenylmethyl)aminobutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0072
-
1-[2-(carboxy)-4-(triphenylmethyl)aminobutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.0078
-
1-[2-(N,N-dimethylaminoethylamido)-4-trityloxybutyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.01
-
1-[2-(tert-butyldiphenylsilyloxyethylamido)-4-trityloxybutyl]uracil Ki above 0.01 mM, pH and temperature not specified in the publication Plasmodium falciparum
0.02
-
1-[2-(diethylamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum
0.098
-
1-[2-(N-benzyloxycarbonylpiperazinamido)-4-(tert-butyldiphenylsilyloxy)butyl]uracil pH and temperature not specified in the publication Plasmodium falciparum

General Information

General Information Comment Organism
physiological function the enzyme is involved in nucleotide metabolism that acts as first line of defence against uracil incorporation into DNA Plasmodium falciparum