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Literature summary for 2.1.1.6 extracted from

  • Nagai, M.; Conney, A.H.; Zhu, B.T.
    Strong inhibitory effects of common tea catechins and bioflavonoids on the O-methylation of catechol estrogens catalyzed by human liver cytosolic catechol-O-methyltransferase (2004), Drug Metab. Dispos., 32, 497-504.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(-)-epigallocatechin-3-O-gallate IC50: 0.05-0.07 nM for the O-methylation of 2-hydroxyestradiol, IC50: 200-500 nM for O-methylation of 4-hydroxyestradiol Homo sapiens
catechin IC50: 14-17 nM for the O-methylation of 2-hydroxyestradiol, IC50: 0.005-0.007 mM for O-methylation of 4-hydroxyestradiol Homo sapiens
epicatechin IC50: 44-65 nM for the O-methylation of 2-hydroxyestradiol, IC50: 0.01-0.018 mM for O-methylation of 4-hydroxyestradiol Homo sapiens
fisetin IC50: 0.0033-0.0045 nM for the O-methylation of 2-hydroxyestradiol, IC50: 0.0026-0.0042 nM for O-methylation of 4-hydroxyestradiol Homo sapiens
quercetin IC50: 0.0009-0.0015 mM for the O-methylation of 2-hydroxyestradiol, IC50: 0.0005-0.0012 mM for O-methylation of 4-hydroxyestradiol Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-adenosyl-L-methionine + 2-hydroxyestradiol
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?
S-adenosyl-L-methionine + 4-hydroxyestradiol
-
Homo sapiens S-adenosyl-L-homocysteine + ?
-
?

Synonyms

Synonyms Comment Organism
COMT
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00004 0.00007 IC50: 0.04-0.07 microM for the O-methylation of 2-hydroxyestradiol Homo sapiens (-)-epigallocatechin-3-O-gallate
0.00037 0.00046 IC50: 0.37-0.46 microM for O-methylation of 4-hydroxyestradiol Homo sapiens (-)-epigallocatechin-3-O-gallate
0.0005 0.0012 IC50: 0.0009-0.0015 mM for the O-methylation of 2-hydroxyestradiol, IC50: 0.0005-0.0012 mM for O-methylation of 4-hydroxyestradiol Homo sapiens quercetin
0.0026 0.0042 IC50: 0.0026-0.0042 mM for O-methylation of 4-hydroxyestradiol Homo sapiens fisetin
0.0033 0.0045 IC50: 0.0033-0.0045 mM for the O-methylation of 2-hydroxyestradiol Homo sapiens fisetin
0.005 0.007 IC50: 14-17 nM for the O-methylation of 2-hydroxyestradiol, IC50: 0.005-0.007 mM for O-methylation of 4-hydroxyestradiol Homo sapiens catechin
0.01 0.018 IC50: 44-65 nM for the O-methylation of 2-hydroxyestradiol, IC50: 0.01-0.018 mM for O-methylation of 4-hydroxyestradiol Homo sapiens epicatechin