BRENDA - Enzyme Database show

Inhibition of steroid sulphatase activity via the percutaneous route: a new option for breast cancer therapy

Purohit, A.; Chander, S.K.; Woo, L.W.; Parsons, M.F.; Jhalli, R.; Potter, B.V.; Reed, M.J.; Anticancer Res. 28, 1517-1523 (2008)

Data extracted from this reference:

Inhibitors
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
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
3.1.6.2
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
3.1.6.2
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)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
Mus musculus
-
dehydroepiandrosterone + sulfate
subsequent conversion to testosterone or aromatisation to estrone
-
?
3.1.6.2
estrone sulfate + H2O
Mus musculus
-
estrone + sulfate
subsequent conversion to estradiol
-
?
Organism
EC Number
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
3.1.6.2
Mus musculus
-
athymic female MF-1 nude mice
-
Source Tissue
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
liver
-
Mus musculus
-
3.1.6.2
skin
-
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
dehydroepiandrosterone sulfate + H2O
-
690451
Mus musculus
dehydroepiandrosterone + sulfate
subsequent conversion to testosterone or aromatisation to estrone
-
-
?
3.1.6.2
estrone sulfate + H2O
-
690451
Mus musculus
estrone + sulfate
subsequent conversion to estradiol
-
-
?
Inhibitors (protein specific)
EC Number
Inhibitors
Commentary
Organism
Structure
3.1.6.2
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
3.1.6.2
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
3.1.6.2
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) (protein specific)
EC Number
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
3.1.6.2
dehydroepiandrosterone sulfate + H2O
Mus musculus
-
dehydroepiandrosterone + sulfate
subsequent conversion to testosterone or aromatisation to estrone
-
?
3.1.6.2
estrone sulfate + H2O
Mus musculus
-
estrone + sulfate
subsequent conversion to estradiol
-
?
Source Tissue (protein specific)
EC Number
Source Tissue
Commentary
Organism
Textmining
3.1.6.2
liver
-
Mus musculus
-
3.1.6.2
skin
-
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
dehydroepiandrosterone sulfate + H2O
-
690451
Mus musculus
dehydroepiandrosterone + sulfate
subsequent conversion to testosterone or aromatisation to estrone
-
-
?
3.1.6.2
estrone sulfate + H2O
-
690451
Mus musculus
estrone + sulfate
subsequent conversion to estradiol
-
-
?