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Literature summary for 3.1.6.2 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

Application Comment Organism
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

Inhibitors Comment Organism Structure
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-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
estrone-3-O-sulfamate
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
ovariectomised female Wistar rats
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
STS
-
Rattus norvegicus

Temperature Optimum [°C]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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