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Literature summary for 3.1.6.2 extracted from

  • Shields-Botella, J.; Bonnet, P.; Duc, I.; Duranti, E.; Meschi, S.; Cardinali, S.; Prouheze, P.; Chaigneau, A.M.; Duranti, V.; Gribaudo, S.; Riviere, A.; Mengual, L.; Carniato, D.; Cecchet, L.; Lafay, J.; Rondot, B.; Sandri, J.; Pascal, J.C.; Delansorne, R.
    In vitro and in vivo models for the evaluation of new inhibitors of human steroid sulfatase, devoid of residual estrogenic activity (2003), J. Steroid Biochem. Mol. Biol., 84, 327-335.
    View publication on PubMed

Application

Application Comment Organism
medicine estrone sulfatase inhibitors can be used as drugs for the treatment of estrogen-dependent breast cancer Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate 6,6,7-COUMATE, IC50: 5.1 nM in JEG-3 cells, 0.43 nM in MCF-7 cells Homo sapiens
6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate 6,6,7-COUMATE, potent inhibitor, in vivo inhibition study, more inhibitory than TX-1299 Rattus norvegicus
estrone-3-sulfamate best inhibitor, IC50: 3.2 nM in JEG-3 cells, 0.08 nM in MCF-7 cells Homo sapiens
additional information not inhibited by danazol or letrozole Homo sapiens
TX-1299 non-steroid Theramex compound, strong inhibitor, IC50: 5.3 nM in JEG-3 cells, 0.76 nM in MCF-7 cells Homo sapiens
TX-1299 non-steroid Theramex compound, potent inhibitor, in vivo inhibition study, 80% as inhibitory as 6,6,7-COUMATE Rattus norvegicus
TX-1492 non-steroid Theramex compound, strong inhibitor, IC50: 22.5 nM in JEG-3 cells, 0.07 nM in MCF-7 cells Homo sapiens
TX-1506 non-steroid Theramex compound, strong inhibitor, IC50: 11.9 nM in JEG-3 cells, 0.06 nM in MCF-7 cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
adult Wistar female ovariectomized rats
-

Source Tissue

Source Tissue Comment Organism Textmining
JEG-3 cell choriocarcinoma cell, more than 80times higher enzyme activity than in MCF-7 cells Homo sapiens
-
MCF-7 cell breast adenocarcinoma cell, more than 80times lower enzyme activity than in JEG-3 cells Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone sulfate + H2O
-
Homo sapiens estrone + sulfate
-
?
estrone sulfate + H2O
-
Rattus norvegicus estrone + sulfate
-
?

Synonyms

Synonyms Comment Organism
estrone sulfatase
-
Homo sapiens
estrone sulfatase
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000006
-
non-steroid Theramex compound, strong inhibitor, 0.06 nM in MCF-7 cells Homo sapiens TX-1506
0.00000008
-
IC50 0.08 nM in MCF-7 cells Homo sapiens estrone-3-sulfamate
0.00000043
-
IC50 0.43 nM in MCF-7 cells Homo sapiens 6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate
0.00000076
-
non-steroid Theramex compound, strong inhibitor, 0.76 nM in MCF-7 cells Homo sapiens TX-1299
0.0000032
-
best inhibitor, IC50: 3.2 nM in JEG-3 cells Homo sapiens estrone-3-sulfamate
0.0000051
-
6,6,7-COUMATE, IC50: 5.1 nM in JEG-3 cells Homo sapiens 6-oxo-8,9,10,11-tetrahydro-7H-cyclohepta-[c][1]benzopyran-3-O-sulfamate
0.0000053
-
non-steroid Theramex compound, strong inhibitor, IC50: 5.3 nM in JEG-3 cells Homo sapiens TX-1299
0.0000119
-
non-steroid Theramex compound, strong inhibitor, IC50: 11.9 nM in JEG-3 cells Homo sapiens TX-1506
0.0000225
-
non-steroid Theramex compound, strong inhibitor, IC50: 22.5 nM in JEG-3 cells Homo sapiens TX-1492