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Literature summary for 3.1.6.2 extracted from
- Anticancer steroid sulfatase inhibitors: synthesis of a potent fluorinated second-generation agent, in vitro and in vivo activities, molecular modeling, and protein crystallography (2008), Mol. Cancer Ther., 7, 2435-2444.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 3-sulfamoyloxy-N-3,3,3-trifluoropropyl-16,17-seco-estra-1,3,4(10)-triene-16,17-imide | highly potent, long-acting, nonestrogenic steroid sulfatase inhibitor with inhibitory properties to human carbonic anhydrase II, thus enabling transport by erythorcytes, no estrogenic effects observed in uterine weight gain study with ovariectomized Wistar rats, 24 h after last dose of 4 days of oral administration of 10 mg/kg/d, in vivo: single dose of 0.1 mg/kg 48% inhibition of liver steroid sulfatase activity, 0.5 and 1 mg/kg total inhibition, activity measured 24 h after dose administration, recovery of steroid sulfatase acitivity after single oral dose of 10 mg/kg: complete inhibition till day 5, day 17: 50% recovery, day 28: complete recovery | Homo sapiens |  |
| 3-sulfamoyloxy-N-3,3,3-trifluoropropyl-16,17-seco-estra-1,3,4(10)-triene-16,17-imide | highly potent, long-acting, nonestrogenic steroid sulfatase inhibitor with inhibitory properties to human carbonic anhydrase II, thus enabling transport by erythorcytes, no estrogenic effects observed in uterine weight gain study with ovariectomized Wistar rats, 24 h after last dose of 4 days of oral administration of 10 mg/kg/d, in vivo: single dose of 0.1 mg/kg 48% inhibition of liver steroid sulfatase activity, 0.5 and 1 mg/kg total inhibition, activity measured 24 h after dose administration, recovery of steroid sulfatase acitivity after single oral dose of 10 mg/kg: complete inhibition till day 5, day 17: 50% recovery, day 28: complete recovery | Rattus norvegicus | |
| STX213 | highly potent, long-acting, nonestrogenic steroid sulfatase inhibitor with inhibitory properties to human carbonic anhydrase II, thus enabling transport by erythorcytes, no estrogenic effects observed in uterine weight gain study with ovariectomized Wistar rats, 24 h after last dose of 4 days of oral administration of 10 mg/kg/d, in vivo: single dose of 0.1 mg/kg 25% inhibition of liver steroid sulfatase activity, 0.5 and 1 mg/kg total inhibition, activity measured 24 h after dose administration, recovery of steroid sulfatase acitivity after single oral dose of 10 mg/kg: complete inhibition till day 4, day 12: 50% recovery, day 15: almost complete recovery | Homo sapiens | |
| STX213 | highly potent, long-acting, nonestrogenic steroid sulfatase inhibitor with inhibitory properties to human carbonic anhydrase II, thus enabling transport by erythorcytes, no estrogenic effects observed in uterine weight gain study with ovariectomized Wistar rats, 24 h after last dose of 4 days of oral administration of 10 mg/kg/d, in vivo: single dose of 0.1 mg/kg 25% inhibition of liver steroid sulfatase activity, 0.5 and 1 mg/kg total inhibition, activity measured 24 h after dose administration, recovery of steroid sulfatase acitivity after single oral dose of 10 mg/kg: complete inhibition till day 4, day 12: 50% recovery, day 15: almost complete recovery | Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| dehydroepiandrosterone sulfate + H2O | Rattus norvegicus | - |
dehydroepiandrosterone + sulfate | conversion to androstenediol by 17beta-hydroxysteroid dehydrogenase type 1, androstenediol supports mammary tumor growth in rodents, or conversion to androstenedione, main substrate for aromatase in postmenopausal women | ? | |
| dehydroepiandrosterone sulfate + H2O | Homo sapiens | - |
dehydroepiandrosterone + sulfate | conversion to androstenediol by 17beta-hydroxysteroid dehydrogenase type 1, androstenediol supports mammary tumor growth in rodents, or conversion to androstenedione, main substrate for aromatase in postmenopausal women | ? | |
| estrone sulfate + H2O | Rattus norvegicus | - |
estrone + sulfate | conversion to estradiol by 17beta-hydroxysteroid dehydrogenase type 1 | ? | |
| estrone sulfate + H2O | Homo sapiens | - |
estrone + sulfate | conversion to estradiol by 17beta-hydroxysteroid dehydrogenase type 1 | ? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | P08842 | - |
- |
| Rattus norvegicus | - |
female adult Wistar rats | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| JEG-3 cell | choriocarcinoma cell line | Homo sapiens | - |
| liver | - |
Rattus norvegicus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| dehydroepiandrosterone sulfate + H2O | - |
Rattus norvegicus | dehydroepiandrosterone + sulfate | conversion to androstenediol by 17beta-hydroxysteroid dehydrogenase type 1, androstenediol supports mammary tumor growth in rodents, or conversion to androstenedione, main substrate for aromatase in postmenopausal women | ? | |
| dehydroepiandrosterone sulfate + H2O | - |
Homo sapiens | dehydroepiandrosterone + sulfate | conversion to androstenediol by 17beta-hydroxysteroid dehydrogenase type 1, androstenediol supports mammary tumor growth in rodents, or conversion to androstenedione, main substrate for aromatase in postmenopausal women | ? | |
| estrone sulfate + H2O | - |
Rattus norvegicus | estrone + sulfate | conversion to estradiol by 17beta-hydroxysteroid dehydrogenase type 1 | ? | |
| estrone sulfate + H2O | - |
Homo sapiens | estrone + sulfate | conversion to estradiol by 17beta-hydroxysteroid dehydrogenase type 1 | ? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| steroid sulfatase | - |
Rattus norvegicus |
| steroid sulfatase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.000000035 | - |
in vitro JEG-3 cells: 0.001-10000 nmol/l inhibitor and incubation with estrone-3-sulfate, IC50 for human carbonic anhydrase II = 0.000003 mM | Rattus norvegicus | 3-sulfamoyloxy-N-3,3,3-trifluoropropyl-16,17-seco-estra-1,3,4(10)-triene-16,17-imide | |
| 0.000000035 | - |
in vitro JEG-3 cells: 0.001-10000 nmol/l inhibitor and incubation with estrone-3-sulfate, IC50 for human carbonic anhydrase II = 0.000003 mM | Homo sapiens | 3-sulfamoyloxy-N-3,3,3-trifluoropropyl-16,17-seco-estra-1,3,4(10)-triene-16,17-imide | |
| 0.00000018 | - |
in vitro JEG-3 cells: 0.001-10000 nmol/l inhibitor and incubation with estrone-3-sulfate, IC50 for human carbonic anhydrase II = 0.000005 mM | Rattus norvegicus | STX213 | |
| 0.00000018 | - |
in vitro JEG-3 cells: 0.001-10000 nmol/l inhibitor and incubation with estrone-3-sulfate, IC50 for human carbonic anhydrase II = 0.000005 mM | Homo sapiens | STX213 | |
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