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Literature summary extracted from

  • Whittingham, J.L.; Leal, I.; Nguyen, C.; Kasinathan, G.; Bell, E.; Jones, A.F.; Berry, C.; Benito, A.; Turkenburg, J.P.; Dodson, E.J.; Perez, L.M.; Wilkinson, A.J.; Johansson, N.G.; Brun, R.; Gilbert, I.H.; Pacanowska, D.G.; Wilson, K.S.
    dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors (2005), Structure, 13, 329-338.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.6.1.23 drug development dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors Plasmodium falciparum

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.6.1.23 DNA and amino acid sequence determination and analysis, the gene locates on chromosome 11, overexpression in Escherichia coli strain BL21(DE3) Plasmodium falciparum

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.6.1.23 purified recombinant enzyme in complex with inhibitor 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine, X-ray diffraction structure determination and analysis at 2.4 A resolution Plasmodium falciparum

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.1.23 2',3',5'-trideoxy-3'-fluoro-5'-(tritylamino)uridine activity against the parasites with IC50: 0.0053 mM Plasmodium falciparum
3.6.1.23 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine activity against the parasites with IC50: 0.0020 mM, binding structure involving Tyr112, Ile117, Ile108, and Asn103, overview Plasmodium falciparum
3.6.1.23 2',5'-dideoxy-5'-(tritylamino)uridine activity against the parasites with IC50: 0.0045 mM Plasmodium falciparum
3.6.1.23 2'-deoxy-5'-O-(triphenylsilyl)uridine activity against the parasites with IC50: 0.0011 mM Plasmodium falciparum
3.6.1.23 2'-deoxy-5'-O-trityluridine activity against the parasites with IC50: 0.006 mM Plasmodium falciparum
3.6.1.23 2'-deoxy-5'-O-[tris(1-methylethoxy)silyl]uridine activity against the parasites with IC50: 0.013 mM Plasmodium falciparum

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.6.1.23 0.0024
-
dUTP pH 5.7-6.2, recombinant enzyme Plasmodium falciparum

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.6.1.23 intracellular
-
Plasmodium falciparum 5622
-

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.6.1.23 Mg2+
-
Plasmodium falciparum

Natural Substrates/ Products (Substrates)

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

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.6.1.23 recombinant enzyme from Escherichia coli strain BL21(DE3) by cation exchange chromatography, gel filtration, and anion exchange chromatography to near homogeneity Plasmodium falciparum

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.6.1.23 schizont asexual stage Plasmodium falciparum
-
3.6.1.23 trophozoite proliferative intraerythroctic Plasmodium falciparum
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.6.1.23 25.75
-
purified recombinant enzyme 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
-
?
3.6.1.23 dUTP + H2O the enzyme is highly specific for dUTP Plasmodium falciparum dUMP + diphosphate
-
?

Subunits

EC Number Subunits Comment Organism
3.6.1.23 trimer crystal structure Plasmodium falciparum

Synonyms

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

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.6.1.23 5.7 6.2 assay at Plasmodium falciparum

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.6.1.23 0.0002
-
2',5'-dideoxy-5'-(tritylamino)uridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum
3.6.1.23 0.0018
-
2'-deoxy-5'-O-trityluridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum
3.6.1.23 0.0028
-
2'-deoxy-5'-O-(triphenylsilyl)uridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum
3.6.1.23 0.005
-
2',3'-dideoxy-3'-fluoro-5'-O-trityluridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum
3.6.1.23 0.0125
-
2',3',5'-trideoxy-3'-fluoro-5'-(tritylamino)uridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum
3.6.1.23 0.2271
-
2'-deoxy-5'-O-[tris(1-methylethoxy)silyl]uridine pH 5.7-6.2, recombinant enzyme Plasmodium falciparum

pI Value

EC Number Organism Comment pI Value Maximum pI Value
3.6.1.23 Plasmodium falciparum sequence calculation
-
6.5

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.6.1.23 0.0011
-
activity against the parasites with IC50: 0.0011 mM Plasmodium falciparum 2'-deoxy-5'-O-(triphenylsilyl)uridine
3.6.1.23 0.002
-
activity against the parasites with IC50: 0.0020 mM, binding structure involving Tyr112, Ile117, Ile108, and Asn103, overview Plasmodium falciparum 2',3'-dideoxy-3'-fluoro-5'-O-trityluridine
3.6.1.23 0.0045
-
activity against the parasites with IC50: 0.0045 mM Plasmodium falciparum 2',5'-dideoxy-5'-(tritylamino)uridine
3.6.1.23 0.0053
-
activity against the parasites with IC50: 0.0053 mM Plasmodium falciparum 2',3',5'-trideoxy-3'-fluoro-5'-(tritylamino)uridine
3.6.1.23 0.006
-
activity against the parasites with IC50: 0.006 mM Plasmodium falciparum 2'-deoxy-5'-O-trityluridine
3.6.1.23 0.013
-
activity against the parasites with IC50: 0.013 mM Plasmodium falciparum 2'-deoxy-5'-O-[tris(1-methylethoxy)silyl]uridine