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Literature summary for 3.1.6.2 extracted from

  • Purohit, A.; Chander, S.K.; Woo, L.W.; Parsons, M.F.; Jhalli, R.; Potter, B.V.; Reed, M.J.
    Inhibition of steroid sulphatase activity via the percutaneous route: a new option for breast cancer therapy (2008), Anticancer Res., 28, 1517-1523.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
additional information STS inhibitors were developed to treat breast cancer but could also used to treat endometriosis, polycystic ovarian disease, prostate cancer, and some androgen-dependent skin conditions, such as acne and hirsutism Mus musculus
STX289 N,N-dimethyl 667 COUMATE, analogue of STX64, inhibition 24 h after oral application: 0.1 mg/kg inhibits liver STS by 45%, skin STS by about 39%, 1 and 10 mg/kg inhibit liver STS completely, skin STS almost completely, inhibition 24 h after topical application to neck skin: 0.1 mg/kg inhibits skin and liver STS by <50%, remote skin STS by about 10%, 1and 10 mg/kg inhibit skin STS by 98%, remote skin STS by about 80 and more than 90% respectively, and liver STS by more than 80 and close by 100% respectively Mus musculus
STX64 synonym BN83495, inhibition 24 h after oral application: 0.1 mg/kg body mass inhibits liver STS by 79%, skin STS by about 59%, 1 and 10 mg/kg inhibitis liver STS activity completely, skin STS almost completely, inhibition 24 h after topical application to neck skin: 0.1 mg/kg inhibits skin STS by 95%, remote skin STS by about 33%, liver STS by 45%, 1 and 10 mg/kg inhibits skin STS by 99%, remote skin STS almost completely, and liver STS by about 90% Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
dehydroepiandrosterone sulfate + H2O Mus musculus
-
dehydroepiandrosterone + sulfate subsequent conversion to testosterone or aromatisation to estrone ?
estrone sulfate + H2O Mus musculus
-
estrone + sulfate subsequent conversion to estradiol ?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
athymic female MF-1 nude mice
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Mus musculus
-
skin
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
dehydroepiandrosterone sulfate + H2O
-
Mus musculus dehydroepiandrosterone + sulfate subsequent conversion to testosterone or aromatisation to estrone ?
estrone sulfate + H2O
-
Mus musculus estrone + sulfate subsequent conversion to estradiol ?

Synonyms

Synonyms Comment Organism
steroid sulfatase
-
Mus musculus
STS
-
Mus musculus