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Literature summary extracted from

  • Fischer, D.S.; Chander, S.K.; Woo, L.W.L.; Fenton, J.C.; Purohit, A.; Reed, M.J.; Potter, B.V.L.
    Novel D-ring modified steroid derivatives as potent, non-estrogenic, steroid sulfatase inhibitors with in vivo activity (2003), J. Steroid Biochem. Mol. Biol., 84, 343-349.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.1.6.2 medicine the STS inhibitors 3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide and 3-sulfamoyloxy-N-(1’’-pyridin-3’’-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide are devoid of estrogenic activity and have therapeutic potential for the treatment of hormone-dependent breast cancer Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.6.2 3-sulfamoyloxy-N-(1''-pyridin-3''-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS Rattus norvegicus
3.1.6.2 3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS Rattus norvegicus
3.1.6.2 estrone-3-O-sulfamate
-
 Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
3.1.6.2 Rattus norvegicus
-
 ovariectomised female Wistar rats
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.6.2 liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.6.2 estrone sulfate + H2O
-
 Rattus norvegicus estrone + sulfate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.6.2 STS
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.6.2 37
-
 assay at Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.6.2 0.000001
-
 highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS Rattus norvegicus 3-sulfamoyloxy-N-propyl-16,17-seco-estra-1,3,5(10)-triene-16,17-imide
3.1.6.2 0.000001
-
 highly potent inhibitor, IC50: 1 nM, 18times more inhibitory than estrone-3-O-sulfamate, in vivo inhibition of STS Rattus norvegicus 3-sulfamoyloxy-N-(1''-pyridin-3''-ylmethyl)-16,17-seco-estra-1,3,5(10)-triene-16,17-imide