Inhibitors | Comment | Organism | Structure |
---|---|---|---|
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 | |
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 | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
dehydroepiandrosterone sulfate + H2O | Homo sapiens | - |
dehydroepiandrosterone + sulfate | subsequent conversion to andgrogen testosterone or androstenediol, androgens stimulate growth of prostate cancer cells | ? | |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
HEK-293-EBNA cell | human embryonic kidney carcinoma cell line | Homo sapiens | - |
Ishikawa cell | human endometrial adenocarcinoma cell culture, human Ishikawa cells transplanted into MF-1 ovariectomized naked mouse model | Homo sapiens | - |
JEG-3 cell | choriocarcinoma cell line | Homo sapiens | - |
LNCaP cell | human prostate cancer cells with mutated androgen receptor, as is typical for many human prostate tumors | Homo sapiens | - |
MCF-7 cell | breast cancer cell line | Homo sapiens | - |
OVCAR-3 cell | human ovarian cancer cell line | Homo sapiens | - |
Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
---|---|---|---|
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 | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
dehydroepiandrosterone sulfate + H2O | - |
Homo sapiens | dehydroepiandrosterone + sulfate | subsequent conversion to andgrogen testosterone or androstenediol, androgens stimulate growth of prostate cancer cells | ? | |
dehydroepiandrosterone sulfate + H2O | - |
Homo sapiens | dehydroepiandrosterone + sulfate | subsequent conversion to testosterone | ? | |
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 | ? | |
estrone sulfate + H2O | - |
Homo sapiens | estrone + sulfate | subsequent conversion to estradiol | ? |
Synonyms | Comment | Organism |
---|---|---|
steroid sulfatase | - |
Homo sapiens |
STS | - |
Homo sapiens |