BRENDA - Enzyme Database show

The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer

Foster, P.A.; Woo, L.W.; Potter, B.V.; Reed, M.J.; Purohit, A.; Endocrinology 149, 4035-4042 (2008)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
STX64
synonyms BN83495 or 667Coumate, 1 mg/kg/day given orally, treatment starting at Ishikawa cell tumor size of about 100 cubic mm (intact mice): no significant tumor growth reduction after 35 days of inhibitor treatment. Estradiol sulfate stimulated tumor growth of Ishikawa cells in ovariectomized mice, results after day 28 of inhibitor treatment: 1 mg/kg/day given orally reduces tumor growth by 48%, complete Ishikawa cell tumor STS inhibition, 1 mg/kg given orally once weekly: no tumor growth inhibition, no tumor STS inhibition, 10 mg/kg/day given orally: tumor growth inhibition by 59%, complete tumor STS inhibition
Homo sapiens
3.1.6.2
STX64
synonyms BN83495 or 667Coumate, estradiol sulfate stimulates tumor growth of Ishikawa cells in ovariectomized mice, results after day 28 of inhibitor treatment: 1 mg/kg/day given orally completely inhibits mouse liver STS acitivity, and reduces plasma estradiol by 63%, 1 mg/kg given orally and once weekly inhibits liver STS activity by about 40%, no plasma estradiol reduction, 10 mg/kg given orally and once weekly: complete inhibition of liver STS, and reduction of plasma estradiol by 93%
Mus musculus
Natural Substrates/ Products (Substrates)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
estrone sulfate + H2O
Mus musculus
-
estrone + sulfate
subsequent conversion to estradiol
-
?
3.1.6.2
estrone sulfate + H2O
Homo sapiens
-
estrone + sulfate
subsequent conversion to estradiol
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.1.6.2
Homo sapiens
-
-
-
3.1.6.2
Mus musculus
-
intact, athymic, female MF-1 nude mice (in vivo tumor growth model), ovariectomized, athymic, female MF-1 nude mice (hormone-dependent in vivo tumor growth model)
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
Ishikawa cell
human endometrial adenocarcinoma cells transplanted into athymic MF-1 intact and ovariectomized naked mouse model
Homo sapiens
-
3.1.6.2
liver
MF-1 mice with transplanted Ishikawa cells grown into tumors
Mus musculus
-
3.1.6.2
plasma
MF-1 mice with transplanted Ishikawa cells grown into tumors
Mus musculus
-
Substrates and Products (Substrate)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.1.6.2
estrone sulfate + H2O
-
692082
Mus musculus
estrone + sulfate
subsequent conversion to estradiol
-
-
?
3.1.6.2
estrone sulfate + H2O
-
692082
Homo sapiens
estrone + sulfate
subsequent conversion to estradiol
-
-
?
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
STX64
synonyms BN83495 or 667Coumate, 1 mg/kg/day given orally, treatment starting at Ishikawa cell tumor size of about 100 cubic mm (intact mice): no significant tumor growth reduction after 35 days of inhibitor treatment. Estradiol sulfate stimulated tumor growth of Ishikawa cells in ovariectomized mice, results after day 28 of inhibitor treatment: 1 mg/kg/day given orally reduces tumor growth by 48%, complete Ishikawa cell tumor STS inhibition, 1 mg/kg given orally once weekly: no tumor growth inhibition, no tumor STS inhibition, 10 mg/kg/day given orally: tumor growth inhibition by 59%, complete tumor STS inhibition
Homo sapiens
3.1.6.2
STX64
synonyms BN83495 or 667Coumate, estradiol sulfate stimulates tumor growth of Ishikawa cells in ovariectomized mice, results after day 28 of inhibitor treatment: 1 mg/kg/day given orally completely inhibits mouse liver STS acitivity, and reduces plasma estradiol by 63%, 1 mg/kg given orally and once weekly inhibits liver STS activity by about 40%, no plasma estradiol reduction, 10 mg/kg given orally and once weekly: complete inhibition of liver STS, and reduction of plasma estradiol by 93%
Mus musculus
Natural Substrates/ Products (Substrates) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
estrone sulfate + H2O
Mus musculus
-
estrone + sulfate
subsequent conversion to estradiol
-
?
3.1.6.2
estrone sulfate + H2O
Homo sapiens
-
estrone + sulfate
subsequent conversion to estradiol
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
Ishikawa cell
human endometrial adenocarcinoma cells transplanted into athymic MF-1 intact and ovariectomized naked mouse model
Homo sapiens
-
3.1.6.2
liver
MF-1 mice with transplanted Ishikawa cells grown into tumors
Mus musculus
-
3.1.6.2
plasma
MF-1 mice with transplanted Ishikawa cells grown into tumors
Mus musculus
-
Substrates and Products (Substrate) (protein specific)
EC Number
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
3.1.6.2
estrone sulfate + H2O
-
692082
Mus musculus
estrone + sulfate
subsequent conversion to estradiol
-
-
?
3.1.6.2
estrone sulfate + H2O
-
692082
Homo sapiens
estrone + sulfate
subsequent conversion to estradiol
-
-
?