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Literature summary for 3.1.6.2 extracted from

  • Fournier, D.; Poirier, D.
    Estradiol dimers as a new class of steroid sulfatase reversible inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 693-696.
    View publication on PubMed
Search for more literature for 3.1.6.2

Inhibitors

Inhibitors Comment Organism Structure
(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
(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
(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
(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)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
dehydroepiandrosterone sulfate + H2O Homo sapiens
-
 dehydroepiandrosterone + sulfate subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase ?
estrone sulfate + H2O Homo sapiens
-
 estrone + sulfate subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell human embryonic kidney cells Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dehydroepiandrosterone sulfate + H2O
-
 Homo sapiens dehydroepiandrosterone + sulfate subsequent conversion to estradiol with 3beta-hydroxysteroid dehydrogenase, aromatase and 17beta-hydroxysteroid dehydrogenase ?
estrone sulfate + H2O
-
 Homo sapiens estrone + sulfate subsequent conversion to estradiol with 17beta-hydroxysteroid dehydrogenase ?

Synonyms

Synonyms Comment Organism
steroid sulfatase
-
 Homo sapiens
STS
-
 Homo sapiens