Literature summary for 3.1.6.2 extracted from

Foster, P.A.; Woo, L.W.; Potter, B.V.; Reed, M.J.; Purohit, A.
The use of steroid sulfatase inhibitors as a novel therapeutic strategy against hormone-dependent endometrial cancer (2008), Endocrinology, 149, 4035-4042.

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Inhibitors

Inhibitors	Comment	Organism	Structure
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
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)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
estrone sulfate + H2O	Mus musculus	-	estrone + sulfate	subsequent conversion to estradiol	?
estrone sulfate + H2O	Homo sapiens	-	estrone + sulfate	subsequent conversion to estradiol	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
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

Source Tissue	Comment	Organism	Textmining
Ishikawa cell	human endometrial adenocarcinoma cells transplanted into athymic MF-1 intact and ovariectomized naked mouse model	Homo sapiens	-
liver	MF-1 mice with transplanted Ishikawa cells grown into tumors	Mus musculus	-
plasma	MF-1 mice with transplanted Ishikawa cells grown into tumors	Mus musculus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
estrone sulfate + H2O	-	Mus musculus	estrone + sulfate	subsequent conversion to estradiol	?
estrone sulfate + H2O	-	Homo sapiens	estrone + sulfate	subsequent conversion to estradiol	?

Synonyms

Synonyms	Comment	Organism
steroid sulfatase	-	Mus musculus
steroid sulfatase	-	Homo sapiens
STS	-	Mus musculus
STS	-	Homo sapiens

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Release 2023.1 (January 2023)