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Literature summary for 2.5.1.18 extracted from

  • Chronopoulou, E.; Papageorgiou, A.; Markoglou, A.; Labrou, N.
    Inhibition of human glutathione transferases by pesticides: development of a simple analytical assay for the quantification of pesticides in water (2012), J. Mol. Catal. B, 81, 43-51.
No PubMed abstract available

Cloned(Commentary)

Cloned (Comment) Organism
isozyme GSTA1-1 expression in Escherichia coli strain BL21(DE3), expression of His-tagged isozymes GSTO1-1 and GSTT2-2 in Escherichia coli strain M15[pREP4] Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
dieldrin a potent reversible inhibitor toward hGSTA1-1, mixed-type inhibition, dieldrin binds specifically to the enzyme presumably at a position that partially overlaps with both the G- and H-site, a site distinct from binding of spiromesifen, binding structure overview Homo sapiens
additional information hGSTA1-1 is more susceptible to inhibition by pesticides than other isoenzymes. In silico docking analysis and kinetic inhibition studies, overview Homo sapiens
spiromesifen a potent reversible inhibitor toward hGSTA1-1, mixed-type inhibition, spiromesifen binds specifically to the enzyme presumably at a position that partially overlaps with both the G- and H-site, a site distinct from binding of dieldrin, binding structure overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme hGSTA1-1
-

Purification (Commentary)

Purification (Comment) Organism
recombinant isozyme GSTA1-1 from Escherichia coli strain BL21(DE3) by glutathione affinity chromatography, recombinant His-tagged isozymes GSTO1-1 and GSTT2-2 in Escherichia coli strain M15[pREP4] by nickel affinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-chloro-2,4-dinitrobenzene + glutathione
-
Homo sapiens S-(2,4-dinitrophenyl)glutathione + HCl
-
?
additional information development of analytical quantification assays for pesticides dieldrin and spiromesifen in water with isozyme GSTA1-1, overview Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
hGSTA1-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information kinetic inhibition studies with dieldrin and spiromesifen, overview Homo sapiens
0.0001
-
dieldrin versus 1-chloro-2,4-dinitrobenzene, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens
0.0004
-
spiromesifen versus 1-chloro-2,4-dinitrobenzene, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens
0.0021
-
spiromesifen versus glutathione, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens
0.0023
-
dieldrin versus glutathione, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0121
-
versus glutathione, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens spiromesifen
0.0179
-
versus 1-chloro-2,4-dinitrobenzene, pH 6.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens dieldrin
0.0242
-
versus glutathione, pH 6.5, 20°C, recombinant wild-type GSTA1-1 Homo sapiens spiromesifen
0.0295
-
versus glutathione, pH 7.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens spiromesifen
0.0345
-
versus 1-chloro-2,4-dinitrobenzene, pH 6.5, 25°C, recombinant wild-type GSTA1-1 Homo sapiens dieldrin
0.0472
-
versus 1-chloro-2,4-dinitrobenzene, pH 7.0, 37°C, recombinant wild-type GSTA1-1 Homo sapiens dieldrin
0.0504
-
versus 1-chloro-2,4-dinitrobenzene, pH 7.5, 37°C, recombinant wild-type GSTA1-1 Homo sapiens dieldrin
0.062
-
versus glutathione, pH 7.0, 37°C, recombinant wild-type GSTA1-1 Homo sapiens spiromesifen
0.0795
-
versus glutathione, pH 6.5, 25°C, recombinant wild-type GSTA1-1 Homo sapiens spiromesifen
0.0983
-
versus 1-chloro-2,4-dinitrobenzene, pH 6.5, 20°C, recombinant wild-type GSTA1-1 Homo sapiens dieldrin