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Literature summary extracted from

  • Day, J.M.; Purohit, A.; Tutill, H.J.; Foster, P.A.; Woo, L.W.; Potter, B.V.; Reed, M.J.
    The development of steroid sulfatase inhibitors for hormone-dependent cancer therapy (2009), Ann. N. Y. Acad. Sci., 1155, 80-87.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.6.2 STX213 phenol sulfamate pharmacophore, irreversible total inhibition from 10-1000 nM in Ishikawa cells, in vivo: upon administration of 1 mg/kg body mass/day reduced tumor growth over 28-day period in transplanted Ishikawa cells in MF-1 nude ovariectomized mice in the presence of estradiol sulfate (prerequisite for tumor cell development in ovariectomized mice), abolished liver STS activity, and reduced plasma estradiol levels Homo sapiens
3.1.6.2 STX64 synonym BN83495, phenol sulfamate pharmacophore, irreversible STS inhibition from 10-1000 nM in Ishikawa cells, irreversible inhibition in OVCAR-3 ovarian cancer cells and JEG-3 choriocarcionoma cells at 10µM, irreversible inhibition from 10-1000 nM in LNCaP prostate cancer cells, in vivo: upon administration of 1 mg/kg body mass/day reduced tumor growth over 28-day period in transplanted Ishikawa cells in MF-1 nude ovariectomized mice in the presence of estradiol sulfate (prerequisite for tumor cell development in ovariectomized mice), abolished liver STS activity, and reduced plasma estradiol levels Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.6.2 dehydroepiandrosterone sulfate + H2O Homo sapiens
-
 dehydroepiandrosterone + sulfate subsequent conversion to andgrogen testosterone or androstenediol, androgens stimulate growth of prostate cancer cells ?
3.1.6.2 estrone sulfate + H2O Homo sapiens
-
 estrone + sulfate subsequent conversion to biologically active estrogen estradiol, increased activity and expression of STS in hormone-dependent cancer cells, estradiol prerequisite for Ishikawa cell tumorgenesis in ovariectomized mouse model, estrogens are suggested as growth stimulators in prostate cancer cells as well ?

Organism

EC Number Organism UniProt Comment Textmining
3.1.6.2 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.6.2 HEK-293-EBNA cell human embryonic kidney carcinoma cell line Homo sapiens
-
3.1.6.2 Ishikawa cell human endometrial adenocarcinoma cell culture, human Ishikawa cells transplanted into MF-1 ovariectomized naked mouse model Homo sapiens
-
3.1.6.2 JEG-3 cell choriocarcinoma cell line Homo sapiens
-
3.1.6.2 LNCaP cell human prostate cancer cells with mutated androgen receptor, as is typical for many human prostate tumors Homo sapiens
-
3.1.6.2 MCF-7 cell breast cancer cell line Homo sapiens
-
3.1.6.2 OVCAR-3 cell human ovarian cancer cell line Homo sapiens
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
3.1.6.2 additional information
-
 STS activity in 86% of human endometrial cancer tissue, 26% in normal endometrial tissue in 26%, confirmed by immunohistochemistry, STS acitivity in MCF-7 breast cancer cells about 20 fmol/20 h/million cells, STS acitivity in Ishikawa endometrial cancer cells 39.4 fmol/20 h/million cells, STS acitivity in LNCaP prostate cancer cells 41.5 fmol/20 h/million cells, STS acitivity in OVCAR-3 ovarian cancer cells 127.4 fmol/20 h/million cells Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.6.2 dehydroepiandrosterone sulfate + H2O
-
 Homo sapiens dehydroepiandrosterone + sulfate subsequent conversion to andgrogen testosterone or androstenediol, androgens stimulate growth of prostate cancer cells ?
3.1.6.2 dehydroepiandrosterone sulfate + H2O
-
 Homo sapiens dehydroepiandrosterone + sulfate subsequent conversion to testosterone ?
3.1.6.2 estrone sulfate + H2O
-
 Homo sapiens estrone + sulfate subsequent conversion to biologically active estrogen estradiol, increased activity and expression of STS in hormone-dependent cancer cells, estradiol prerequisite for Ishikawa cell tumorgenesis in ovariectomized mouse model, estrogens are suggested as growth stimulators in prostate cancer cells as well ?
3.1.6.2 estrone sulfate + H2O
-
 Homo sapiens estrone + sulfate subsequent conversion to estradiol ?

Synonyms

EC Number Synonyms Comment Organism
3.1.6.2 steroid sulfatase
-
 Homo sapiens
3.1.6.2 STS
-
 Homo sapiens