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Literature summary for 2.5.1.18 extracted from

  • Wang, J.; Wang, S.; Song, D.; Zhao, D.; Sha, Y.; Jiang, Y.; Jing, Y.; Cheng, M.
    Chalcone derivatives inhibit glutathione S-transferase P1-1 activity: insights into the interaction mode of alpha, beta-unsaturated carbonyl compounds (2009), Chem. Biol. Drug Des., 73, 511-514.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-2-[(4-methoxyphenyl)carbonyl]-3-(2,3,4-trimethoxyphenyl)prop-2-enoic acid
-
Homo sapiens
(2Z)-2-[(4-methylphenyl)carbonyl]-3-(2,3,4-trimethoxyphenyl)prop-2-enoic acid
-
Homo sapiens
(2Z)-2-[(4-methylphenyl)carbonyl]-3-phenylprop-2-enoic acid 8.1% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(1,3-benzodioxol-5-yl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid 10% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(1,3-benzodioxol-5-yl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 9.6% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(2-methylphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 9.3% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid
-
Homo sapiens
(2Z)-3-(3,4-dihydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
Homo sapiens
(2Z)-3-(3-hydroxyphenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid 6.6% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(3-hydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 13.9% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 19.0% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(4-chlorophenyl)-2-[(4-methoxyphenyl)carbonyl]prop-2-enoic acid 14.4% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(4-chlorophenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 14.4% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(4-fluorophenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
Homo sapiens
(2Z)-3-(4-hydroxy-3-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 8.8% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(4-hydroxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 12.5% inhibition at 0.02 mM Homo sapiens
(2Z)-3-(4-methoxyphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
Homo sapiens
(2Z)-3-(4-methylphenyl)-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid
-
Homo sapiens
(2Z)-3-[4-(dimethylamino)phenyl]-2-[(4-methylphenyl)carbonyl]prop-2-enoic acid 9.3% inhibition at 0.02 mM Homo sapiens
Ethacrynic acid 88.6% inhibition at 0.02 mM Homo sapiens
additional information inhibitory potencies of chalcone derivatives on GSTP1-1, molecular modeling, overview. No or poor inhibition by I-02, I-03, I-10, I-13, I-14, I-15, and I-16 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozyme GSTP1-1
-

Source Tissue

Source Tissue Comment Organism Textmining
HL-60 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glutathione + 1-chloro-2,4-dinitrobenzene
-
Homo sapiens S-(2,4-dinitrophenyl)glutathione + HCl
-
?

Synonyms

Synonyms Comment Organism
glutathione S-transferase P1-1
-
Homo sapiens
GSTP1-1
-
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
6.8
-
assay at Homo sapiens

General Information

General Information Comment Organism
metabolism glutathione S-transferase P1-1 is one of the most important members of phase II detoxification enzyme family which catalyzes the conjugation of glutathione with broad substrates such as chemotherapeutic agents Homo sapiens