BRENDA - Enzyme Database show

Estradiol dimers as a new class of steroid sulfatase reversible inhibitors

Fournier, D.; Poirier, D.; Bioorg. Med. Chem. Lett. 19, 693-696 (2009)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
(17beta)-17-(4-tert-butylbenzyl)estra-1(10),2,4-triene-3,17-diol
estradiol phenolic reversible inhibitor as reference, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 39% inhibition, at 1 microM 62% inhibition
Homo sapiens
3.1.6.2
(17beta)-17-benzylestra-1(10),2,4-triene-3,17-diol
estradiol phenolic reversible inhibitor as reference, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 15% inhibition, at 1 microM 48% inhibition
Homo sapiens
3.1.6.2
(17beta,17'beta)-17,17'-(2E)-but-2-ene-1,4-diylbisestra-1(10),2,4-triene-3,17-diol
reversible non-competitive or mixed inhibition, estradiol dimer with C17-C17 bond, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 42% inhibition, at 1 microM 56% inhibition
Homo sapiens
3.1.6.2
(17beta,17'beta)-17,17'-butane-1,4-diylbisestra-1(10),2,4-triene-3,17-diol
reversible non-competitive or mixed inhibition, estradiol dimer with C17-C17 bond, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 30% inhibition, at 1 microM 54% inhibition
Homo sapiens
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
Homo sapiens
-
dehydroepiandrosterone + sulfate
subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase
-
?
3.1.6.2
estrone sulfate + H2O
Homo sapiens
-
estrone + sulfate
subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.1.6.2
Homo sapiens
-
-
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
HEK-293 cell
human embryonic kidney cells
Homo sapiens
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
-
691323
Homo sapiens
dehydroepiandrosterone + sulfate
subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase
-
-
?
3.1.6.2
estrone sulfate + H2O
-
691323
Homo sapiens
estrone + sulfate
subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase
-
-
?
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
(17beta)-17-(4-tert-butylbenzyl)estra-1(10),2,4-triene-3,17-diol
estradiol phenolic reversible inhibitor as reference, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 39% inhibition, at 1 microM 62% inhibition
Homo sapiens
3.1.6.2
(17beta)-17-benzylestra-1(10),2,4-triene-3,17-diol
estradiol phenolic reversible inhibitor as reference, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 15% inhibition, at 1 microM 48% inhibition
Homo sapiens
3.1.6.2
(17beta,17'beta)-17,17'-(2E)-but-2-ene-1,4-diylbisestra-1(10),2,4-triene-3,17-diol
reversible non-competitive or mixed inhibition, estradiol dimer with C17-C17 bond, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 42% inhibition, at 1 microM 56% inhibition
Homo sapiens
3.1.6.2
(17beta,17'beta)-17,17'-butane-1,4-diylbisestra-1(10),2,4-triene-3,17-diol
reversible non-competitive or mixed inhibition, estradiol dimer with C17-C17 bond, possible additional breast cancer therapy, no inhibition at 0.01 microM, at 0.1 microM 30% inhibition, at 1 microM 54% inhibition
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
Homo sapiens
-
dehydroepiandrosterone + sulfate
subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase
-
?
3.1.6.2
estrone sulfate + H2O
Homo sapiens
-
estrone + sulfate
subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
HEK-293 cell
human embryonic kidney cells
Homo sapiens
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
-
691323
Homo sapiens
dehydroepiandrosterone + sulfate
subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase
-
-
?
3.1.6.2
estrone sulfate + H2O
-
691323
Homo sapiens
estrone + sulfate
subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase
-
-
?