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Literature summary extracted from

  • Narwal, M.; Jemth, A.S.; Gustafsson, R.; Almloef, I.; Warpman Berglund, U.; Helleday, T.; Stenmark, P.
    Crystal structures and inhibitor interactions of mouse and dog MTH1 reveal species-specific differences in affinity (2018), Biochemistry, 57, 593-603 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.6.1.56 expressed in Escherichia coli BL21(DE3) cells Mus musculus
3.6.1.56 expressed in Escherichia coli BL21(DE3) cells Canis lupus familiaris

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.6.1.56 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
3.6.1.56 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

EC Number Protein Variants Comment Organism
3.6.1.56 L116M the mutation causes a considerable drop in activity with dGTP compared to the wild type enzyme Mus musculus
3.6.1.56 M116L the mutation causes a considerable drop in activity with dGTP compared to the wild type enzyme Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.1.56 N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine i.e. TH588 Canis lupus familiaris
3.6.1.56 N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine i.e. TH588 Homo sapiens
3.6.1.56 N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine i.e. TH588 Mus musculus
3.6.1.56 TH1579
-
 Canis lupus familiaris
3.6.1.56 TH1579
-
 Homo sapiens
3.6.1.56 TH1579
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.6.1.56 Canis lupus familiaris F1P963
-
-
3.6.1.56 Homo sapiens P36639
-
-
3.6.1.56 Mus musculus P53368
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.6.1.56 HisTrap column chromatography and Superdex 75 gel filtration Mus musculus
3.6.1.56 HisTrap column chromatography and Superdex 75 gel filtration Canis lupus familiaris

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.6.1.56 2-hydroxy-ATP + H2O
-
 Mus musculus 2-hydroxy-AMP + diphosphate
-
 ?
3.6.1.56 2-hydroxy-ATP + H2O
-
 Homo sapiens 2-hydroxy-AMP + diphosphate
-
 ?
3.6.1.56 2-hydroxy-ATP + H2O
-
 Canis lupus familiaris 2-hydroxy-AMP + diphosphate
-
 ?
3.6.1.56 2-hydroxy-dATP + H2O
-
 Mus musculus 2-hydroxy-dAMP + diphosphate
-
 ?
3.6.1.56 2-hydroxy-dATP + H2O
-
 Homo sapiens 2-hydroxy-dAMP + diphosphate
-
 ?
3.6.1.56 2-hydroxy-dATP + H2O
-
 Canis lupus familiaris 2-hydroxy-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dATP + H2O
-
 Mus musculus 8-oxo-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dATP + H2O
-
 Homo sapiens 8-oxo-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dATP + H2O
-
 Canis lupus familiaris 8-oxo-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dGTP + H2O
-
 Mus musculus 8-oxo-dGMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dGTP + H2O
-
 Homo sapiens 8-oxo-dGMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dGTP + H2O
-
 Canis lupus familiaris 8-oxo-dGMP + diphosphate
-
 ?
3.6.1.56 dGTP + H2O
-
 Mus musculus dGMP + diphosphate
-
 ?
3.6.1.56 dGTP + H2O
-
 Homo sapiens dGMP + diphosphate
-
 ?
3.6.1.56 dGTP + H2O
-
 Canis lupus familiaris dGMP + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.6.1.56 MTH1
-
 Mus musculus
3.6.1.56 MTH1
-
 Homo sapiens
3.6.1.56 MTH1
-
 Canis lupus familiaris
3.6.1.56 MutT homologue 1
-
 Mus musculus
3.6.1.56 MutT homologue 1
-
 Homo sapiens
3.6.1.56 MutT homologue 1
-
 Canis lupus familiaris

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.6.1.56 0.0000022
-
 wild type enzyme, at pH 8.0 and 22°C Homo sapiens TH1579
3.6.1.56 0.0000039
-
 wild type enzyme, at pH 8.0 and 22°C Canis lupus familiaris TH1579
3.6.1.56 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
3.6.1.56 0.0000068
-
 wild type enzyme, at pH 8.0 and 22°C Homo sapiens N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine
3.6.1.56 0.0000225
-
 mutant enzyme M116L, at pH 8.0 and 22°C Homo sapiens N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine
3.6.1.56 0.000032
-
 mutant enzyme L116M, at pH 8.0 and 22°C Mus musculus N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine
3.6.1.56 0.000132
-
 wild type enzyme, at pH 8.0 and 22°C Mus musculus TH1579
3.6.1.56 0.000138
-
 wild type enzyme, at pH 8.0 and 22°C Mus musculus N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine