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Literature summary for 2.5.1.18 extracted from

  • Mukanganyama, S.; Bezabih, M.; Robert, M.; Ngadjui, B.T.; Kapche, G.F.; Ngandeu, F.; Abegaz, B.
    The evaluation of novel natural products as inhibitors of human glutathione transferase P1-1 (2011), J. Enzyme Inhib. Med. Chem., 26, 460-467.
    View publication on PubMed
Search for more literature for 2.5.1.18

Cloned(Commentary)

Cloned (Comment) Organism
GSTP1-1 expression in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2R,3S)-2-(3,4-dihydroxyphenyl)-3,4-dihydro-2H-chromene-3,5,7-triol a coumaroflavan from Treculia africana, 26% total inhibition at 0.033 mM Homo sapiens
(4S,6Z,10Z,11aS)-4-ethoxy-6-(hydroxymethyl)-3-methylidene-10-propoxy-3a,4,5,8,9,11a-hexahydrocyclodeca[b]furan-2(3H)-one a sesquiterpene lactone from Dicoma anomala collected from Namibia, 75% total inhibition at 0.033 mM Homo sapiens
1,7-dihydroxyanthracen-9(10H)-one a xanthone from Mammea africana, 21% total inhibition at 0.033 mM Homo sapiens
2-hydroxyanthracen-9(10H)-one a xanthone Mammea from africana, 38% total inhibition at 0.033 mM Homo sapiens
3-(3,4-dihydroxybenzoyl)-4-hydroxy-8-methyl-1,5,7-tris(3-methylbut-2-en-1-yl)-8-(4-methylpent-3-en-1-yl)bicyclo[3.3.1]non-3-ene-2,9-dione a benzophenone Garcinia smeathmannii, 41% total inhibition at 0.033 mM Homo sapiens
3-ethyl-2-oxo-3,3a,7a,9b-tetrahydro-2H,4aH-1,4,5-trioxadicyclopenta[a,hi]indene-7-carboxylic acid an iridoid from Plumeeria rubra, 51% total inhibition at 0.033 mM Homo sapiens
4-[3-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-3-hydroxybutoxy]-7H-furo[3,2-g]chromen-7-one a furocoumarin from Dorstenia elliptica, 34% total inhibition at 0.033 mM Homo sapiens
5,7-dihydroxy-6-(2-hydroxybutanoyl)-8-(3-methylbut-2-en-1-yl)-4-propyl-2H-chromen-2-one a coumarin from Mammea africana, 33% total inhibition at 0.033 mM Homo sapiens
5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione an isofuranonaphthoquinone from Bulbine frutescens, the mode of inhibition is mixed, partial (G site) and noncompetitive (H site), 68% total inhibition at 0.033 mM Homo sapiens
6-butanoyl-5,7-dihydroxy-4-phenyl-2H-chromen-2-one a coumarin from Mammea africana, 23% total inhibition at 0.033 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant GSTP1-1 from Escherichia coli 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
-
 ?
monochlorobimane + glutathione
-
 Homo sapiens bimane-glutathione + HCl
-
 ?
additional information monochlorobimane and 1-chloro-2,4-dinitrobenzene are used to determine GST activity Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
glutathione transferase P1-1
-
 Homo sapiens
GST
-
 Homo sapiens
GSTP1-1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00021
-
 5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione inhibition H site, pH and temperature not specified in the publication Homo sapiens
0.0088
-
 5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione inhibition G site, pH and temperature not specified in the publication Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0068
-
 pH and temperature not specified in the publication Homo sapiens 5,8-dihydroxy-1-(hydroxymethyl)naphtho[2,3-c]furan-4,9-dione