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Literature summary for 2.5.1.18 extracted from

  • Koutsoumpli, G.E.; Dimaki, V.D.; Thireou, T.N.; Eliopoulos, E.E.; Labrou, N.E.; Varvounis, G.I.; Clonis, Y.D.
    Synthesis and study of 2-(pyrrolesulfonylmethyl)-N-arylimines: a new class of inhibitors for human glutathione transferase A1-1 (2012), J. Med. Chem., 55, 6802-6813.
    View publication on PubMed
Search for more literature for 2.5.1.18

Cloned(Commentary)

Cloned (Comment) Organism
expression of isozyme GSTA1-1 in Escherichia coli strain BL21 (DE3) Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-methyl-2-[((2-nitrobenzyl)sulfonyl)]-1H-pyrrole 44.3% inhibition at 0.1 mM Homo sapiens
1-methyl-2-[(2-nitrobenzyl)sulfanyl]-1H-pyrrole
-
 Homo sapiens
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-((1E)-[4-(trifluoromethyl)phenyl]methylene)aniline 68.4% inhibition at 0.1 mM Homo sapiens
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(4-nitrophenyl)methylene]aniline 90.0% inhibition at 0.1 mM Homo sapiens
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(phenyl)methylene]aniline 30.2% inhibition at 0.1 mM Homo sapiens
2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-1H-pyrrol-2-ylmethylene]aniline 36.0% inhibition at 0.1 mM Homo sapiens
2-[(1-methyl-1H-pyrrol-2-ylsulfonyl)methyl]aniline 28.0% inhibition at 0.1 mM Homo sapiens
bromosulfophthalein
-
 Homo sapiens
additional information synthesis, screening, and potencies of 2-(pyrrolesulfonylmethyl)-N-arylimines as inhibitors of human glutathione transferase A1-1, in silico molecular docking analysis and molecular modeling, overview Homo sapiens
N-((1E)-[4-(dimethylamino)phenyl]methylene)-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline 78.9% inhibition at 0.1 mM Homo sapiens
N-[(1E)-(2-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline 88.8% inhibition at 0.1 mM Homo sapiens
N-[(1E)-(4-chlorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline 60.4% inhibition at 0.1 mM Homo sapiens
N-[(1E)-(4-fluorophenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline 37.1% inhibition at 0.1 mM Homo sapiens
N-[(1E)-(5-bromo-2-methoxyphenyl)methylene]-2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)aniline 646% inhibition at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 isozyme GSTA1-1
-

Purification (Commentary)

Purification (Comment) Organism
recombinant isozyme GSTA1-1 from Escherichia coli strain BL21 (DE3) by glutathione 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 2,4-dinitrophenyl-glutathione + HCl
-
 ?

Synonyms

Synonyms Comment Organism
GSTA1-1
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 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 inhibition kinetics of 2-(pyrrolesulfonylmethyl)-N-arylimines versus substrate 1-chloro-2,4-dinitrobenzene on GSTA1-1, overview Homo sapiens
0.071
-
 2-([(1-methyl-1H-pyrrol-2-yl)sulfonyl]methyl)-N-[(1E)-(4-nitrophenyl)methylene]aniline pH 6.5, 25°C Homo sapiens

General Information

General Information Comment Organism
physiological function overexpression of human GSTA1-1 in tumor cells is part of multi drug resistance mechanisms Homo sapiens