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Literature summary extracted from

  • Larsson, A.K.; Shokeer, A.; Mannervik, B.
    Molecular evolution of theta-class glutathione transferase for enhanced activity with the anticancer drug 1,3-bis-(2-chloroethyl)-1-nitrosourea and other alkylating agents (2010), Arch. Biochem. Biophys., 497, 28-34.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.5.1.18 medicine GSTs catalyzing inactivation of anticancer drugs may find clinical use in protecting sensitive normal tissues to toxic side effects in treated patients, and as selectable markers in gene therapy Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.5.1.18 recombinant expression of the His6-tagged isozyme GST T1-1 in Escherichia coli Mus musculus
2.5.1.18 recombinant expression of the His6-tagged wild-type and mutant isozymes GST T1-1 in Escherichia coli Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.5.1.18 C14S/T226I/W234R construction of chimeric mutant F2:1215 comprising sequences from the human isozymes GST-T1-1 and GST-T2, as well as from the GST-T1-1 of Mus musculus, the mutant F2:1215 shows highly increased activity compared to the human enzyme and increased activity compared to the murine enzyme, overview Homo sapiens
2.5.1.18 additional information construction of chimeric mutants F2:1215 and F5:1474 comprising sequences from the murine isozymes GST-T1-1, as well as from the isozymes GST-T1-1 and GST-T2 of Homo sapiens, the mutant F2:1215 and mutant F5:1474 show increased activity compared to the human and to the murine enzyme, overview Mus musculus
2.5.1.18 W234R construction of chimeric mutant F5:1474 comprising sequences from the human isozymes GST-T1-1 and GST-T2, as well as from the GST-T1-1 of Mus musculus, the mutant F5:1474 shows increased activity compared to the human enzyme and to the murine enzyme, overview Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.5.1.18 additional information
-
additional information steady-state kinetics of recombinant His6-tagged isozyme GST T1-1, substrate 1,3-bis-(2-chloroethyl)-1-nitrosourea Mus musculus
2.5.1.18 additional information
-
additional information steady-state kinetics of recombinant His6-tagged wild-type and mutant isozymes GST T1-1, substrate 1,3-bis-(2-chloroethyl)-1-nitrosourea Homo sapiens
2.5.1.18 0.6
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Mus musculus
2.5.1.18 0.6
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Homo sapiens
2.5.1.18 0.8
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Mus musculus
2.5.1.18 1
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.5.1.18 additional information Homo sapiens the human isozyme GST T1-1 is 80fold less active than the murine isozyme GST T1-1 ?
-
?
2.5.1.18 additional information Mus musculus the murine isozyme GST T1-1 is 80fold more active than the human isozyme GST T1-1 ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.5.1.18 Homo sapiens
-
isozyme GST T1-1
-
2.5.1.18 Mus musculus
-
isozyme GST T1-1
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.5.1.18 1,2-epoxy-3-(4-nitrophenoxy)-propane + glutathione
-
Mus musculus ?
-
?
2.5.1.18 1,2-epoxy-3-(4-nitrophenoxy)-propane + glutathione
-
Homo sapiens ?
-
?
2.5.1.18 1,3-bis-(2-chloroethyl)-1-nitrosourea + glutathione
-
Mus musculus ?
-
?
2.5.1.18 1,3-bis-(2-chloroethyl)-1-nitrosourea + glutathione
-
Homo sapiens ?
-
?
2.5.1.18 4-nitrophenethyl bromide + glutathione
-
Mus musculus ?
-
?
2.5.1.18 4-nitrophenethyl bromide + glutathione
-
Homo sapiens ?
-
?
2.5.1.18 additional information the human isozyme GST T1-1 is 80fold less active than the murine isozyme GST T1-1 Homo sapiens ?
-
?
2.5.1.18 additional information the murine isozyme GST T1-1 is 80fold more active than the human isozyme GST T1-1 Mus musculus ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.5.1.18 GST T1-1
-
Mus musculus
2.5.1.18 GST T1-1
-
Homo sapiens
2.5.1.18 theta-class glutathione transferase
-
Mus musculus
2.5.1.18 theta-class glutathione transferase
-
Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.5.1.18 37
-
assay at Mus musculus
2.5.1.18 37
-
assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.5.1.18 0.035
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Homo sapiens
2.5.1.18 2.3
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Mus musculus
2.5.1.18 3.6
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Mus musculus
2.5.1.18 3.6
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.5.1.18 7.4
-
assay at Mus musculus
2.5.1.18 7.4
-
assay at Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.5.1.18 0.036
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Homo sapiens
2.5.1.18 2.9
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant wild-type isozyme GST-T1-1 Mus musculus
2.5.1.18 6.3
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Mus musculus
2.5.1.18 6.3
-
1,3-Bis-(2-chloroethyl)-1-nitrosourea pH 7.4, 37°C, recombinant mutant F2:1215 Homo sapiens