Application | Comment | Organism |
---|---|---|
medicine | the enzyme is an excellent target for chemotherapy with 6-substituted purine nucleosides being potential selective antitoxoplasmic agents | Toxoplasma gondii |
Cloned (Comment) | Organism |
---|---|
overexpression of the soluble enzyme in Escherichia coli strain BL21(DE3) | Toxoplasma gondii |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2,4,6-trimethyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
2,4-dichloro-6-benzylthioinosine | - |
Toxoplasma gondii | |
2-chloro-6-benzylthioinosine | - |
Toxoplasma gondii | |
2-chloro-6-fluoro-6-benzylthioinosine | - |
Toxoplasma gondii | |
2-fluoro-6-benzylthioinosine | - |
Toxoplasma gondii | |
2-methyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
3,4-dichloro-6-benzylthioinosine | - |
Toxoplasma gondii | |
3-methyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
3-nitro-6-benzylthioinosine | - |
Toxoplasma gondii | |
3-trifluoromethyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-acetoxy-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-bromo-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-chloro-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-cyano-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-fluoro-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-methoxy-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-methyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-nitro-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-tert-butyl-6-benzylthioinosine | - |
Toxoplasma gondii | |
4-trifluoromethoxy-6-benzylthioinosine | - |
Toxoplasma gondii | |
6-benzylthioinosine | - |
Toxoplasma gondii | |
additional information | IC50 values and toxicities, i.e. rates of survival, of the 6-benzylthioinosine derivatives in wild-type strain RH and in the mutant strain TgAK-3 in human fibrobalsts, effects of 6-benzylthioinosine and derivatives 2-cyano-6-benzylthioinosine and 2,4-dichloro-6-benzylthioinosine on survival of mice infected with the wild-type strain RH, overview | Toxoplasma gondii | |
pyrimethamine | - |
Toxoplasma gondii | |
Sulfadiazine | - |
Toxoplasma gondii |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | at 5 mM MgCl2 | Toxoplasma gondii |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
75000 | - |
x * 75000, about, recombinant enzyme | Toxoplasma gondii |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + adenosine | Toxoplasma gondii | enzyme shows highest activity of all enzymes involved in the adenosine salvage metabolism | ADP + AMP | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Toxoplasma gondii | - |
wild-type strain RH and enzyme-deficient mutant strain TgAK-3, cultured in mice or human fibroblasts | - |
Purification (Comment) | Organism |
---|---|
recombinant enzyme from Escherichia coli strain BL21(DE3) by 3 steps of ion exchange chromatography, to homogeneity | Toxoplasma gondii |
Storage Stability | Organism |
---|---|
-75°C, pure enzyme, 20 mM Tris-HCl, pH 8.0, 15 mM 2-mercaptoethanol, stable for months | Toxoplasma gondii |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + adenosine | - |
Toxoplasma gondii | ADP + AMP | - |
? | |
ATP + adenosine | enzyme shows highest activity of all enzymes involved in the adenosine salvage metabolism | Toxoplasma gondii | ADP + AMP | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 75000, about, recombinant enzyme | Toxoplasma gondii |
Synonyms | Comment | Organism |
---|---|---|
AK | - |
Toxoplasma gondii |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Toxoplasma gondii |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Toxoplasma gondii |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0007 | - |
2,4-dichloro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0009 | - |
4-cyano-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0011 | - |
4-nitro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0012 | - |
4-fluoro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0013 | - |
3-methyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0014 | - |
2-chloro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0015 | - |
2-methyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0021 | - |
4-chloro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0024 | - |
6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0025 | - |
3,4-dichloro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0026 | - |
4-methoxy-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0029 | - |
3-trifluoromethyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.003 | - |
3-nitro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0033 | - |
4-methyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0075 | - |
4-bromo-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.0377 | - |
2-chloro-6-fluoro-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.096 | - |
4-acetoxy-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.113 | - |
4-tert-butyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.141 | - |
4-trifluoromethoxy-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii | |
0.15 | - |
2,4,6-trimethyl-6-benzylthioinosine | pH 7.4, 37°C, recombinant enzyme | Toxoplasma gondii |