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Literature summary for 3.6.1.56 extracted from
- Crystal structures and inhibitor interactions of mouse and dog MTH1 reveal species-specific differences in affinity (2018), Biochemistry, 57, 593-603 .
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in Escherichia coli BL21(DE3) cells | Mus musculus |
| expressed in Escherichia coli BL21(DE3) cells | Canis lupus familiaris |
Crystallization (Commentary)
| Crystallization (Comment) | Organism |
|---|---|
| in complex with inhibitor TH588, sitting drop vapor diffusion method, using 200 mM potassium thiocyanate and 20% (w/v) PEG 3350. In complex with substrate 8-oxo-dGTP, sitting drop vapor diffusion method, using 200 mM ammonium nitrate, 34% (w/v) PEG 3350, and 10 mM copper(II) chloride dihydrate | Mus musculus |
| sitting drop vapor diffusion method, using 100 mM sodium acetate (pH 3.5), 200 mM Li2SO4, 0.5% (w/v) noctyl beta-D-glucoside, and 34% (w/v) PEG 6000 | Canis lupus familiaris |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| L116M | the mutation causes a considerable drop in activity with dGTP compared to the wild type enzyme | Mus musculus |
| M116L | the mutation causes a considerable drop in activity with dGTP compared to the wild type enzyme | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | i.e. TH588 | Canis lupus familiaris |  |
| N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | i.e. TH588 | Homo sapiens | |
| N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | i.e. TH588 | Mus musculus | |
| TH1579 | - |
Canis lupus familiaris | |
| TH1579 | - |
Homo sapiens | |
| TH1579 | - |
Mus musculus |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Canis lupus familiaris | F1P963 | - |
- |
| Homo sapiens | P36639 | - |
- |
| Mus musculus | P53368 | - |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| HisTrap column chromatography and Superdex 75 gel filtration | Mus musculus |
| HisTrap column chromatography and Superdex 75 gel filtration | Canis lupus familiaris |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2-hydroxy-ATP + H2O | - |
Mus musculus | 2-hydroxy-AMP + diphosphate | - |
? | |
| 2-hydroxy-ATP + H2O | - |
Homo sapiens | 2-hydroxy-AMP + diphosphate | - |
? | |
| 2-hydroxy-ATP + H2O | - |
Canis lupus familiaris | 2-hydroxy-AMP + diphosphate | - |
? | |
| 2-hydroxy-dATP + H2O | - |
Mus musculus | 2-hydroxy-dAMP + diphosphate | - |
? | |
| 2-hydroxy-dATP + H2O | - |
Homo sapiens | 2-hydroxy-dAMP + diphosphate | - |
? | |
| 2-hydroxy-dATP + H2O | - |
Canis lupus familiaris | 2-hydroxy-dAMP + diphosphate | - |
? | |
| 8-oxo-dATP + H2O | - |
Mus musculus | 8-oxo-dAMP + diphosphate | - |
? | |
| 8-oxo-dATP + H2O | - |
Homo sapiens | 8-oxo-dAMP + diphosphate | - |
? | |
| 8-oxo-dATP + H2O | - |
Canis lupus familiaris | 8-oxo-dAMP + diphosphate | - |
? | |
| 8-oxo-dGTP + H2O | - |
Mus musculus | 8-oxo-dGMP + diphosphate | - |
? | |
| 8-oxo-dGTP + H2O | - |
Homo sapiens | 8-oxo-dGMP + diphosphate | - |
? | |
| 8-oxo-dGTP + H2O | - |
Canis lupus familiaris | 8-oxo-dGMP + diphosphate | - |
? | |
| dGTP + H2O | - |
Mus musculus | dGMP + diphosphate | - |
? | |
| dGTP + H2O | - |
Homo sapiens | dGMP + diphosphate | - |
? | |
| dGTP + H2O | - |
Canis lupus familiaris | dGMP + diphosphate | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MTH1 | - |
Mus musculus |
| MTH1 | - |
Homo sapiens |
| MTH1 | - |
Canis lupus familiaris |
| MutT homologue 1 | - |
Mus musculus |
| MutT homologue 1 | - |
Homo sapiens |
| MutT homologue 1 | - |
Canis lupus familiaris |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000022 | - |
wild type enzyme, at pH 8.0 and 22°C | Homo sapiens | TH1579 | |
| 0.0000039 | - |
wild type enzyme, at pH 8.0 and 22°C | Canis lupus familiaris | TH1579 | |
| 0.000004 | - |
wild type enzyme, at pH 8.0 and 22°C | Canis lupus familiaris | N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | |
| 0.0000068 | - |
wild type enzyme, at pH 8.0 and 22°C | Homo sapiens | N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | |
| 0.0000225 | - |
mutant enzyme M116L, at pH 8.0 and 22°C | Homo sapiens | N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | |
| 0.000032 | - |
mutant enzyme L116M, at pH 8.0 and 22°C | Mus musculus | N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | |
| 0.000132 | - |
wild type enzyme, at pH 8.0 and 22°C | Mus musculus | TH1579 | |
| 0.000138 | - |
wild type enzyme, at pH 8.0 and 22°C | Mus musculus | N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine | |
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