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Literature summary for 3.1.6.2 extracted from

  • Fournier, D.; Poirier, D.
    Chemical synthesis and evaluation of 17alpha-alkylated derivatives of estradiol as inhibitors of steroid sulfatase (2011), Eur. J. Med. Chem., 46, 4227-4237.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure analysis of placenta microsome enzyme, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(17beta)-17-(2,3,4,5,6-pentafluorobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(2-furylmethyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3,5-dibromobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3-benzyloxybenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3-bromobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3-iodobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3-tert-butylbenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(3-trifluoromethylbenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(4-bromobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(4-iodobenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(4-methyl-2-thienyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(4-tert-butylbenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(4-trifluoromethylbenzyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(cyclohexylmethyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(cyclopropylmethyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-(pyridin-3-ylmethyl)-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-benzyl-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-[3,5-bis(benzyloxy)benzyl]-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-[3,5-bis(tert-butyl)benzyl]-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-[3,5-bis(trifluoromethyl)benzyl]-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-[3-(dibenzylamino)benzyl]-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-[4-(benzyloxy)benzyl]-estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
(17beta)-17-{[2-(2-bromoethyl)cyclopropyl]methyl}estra-1(10),2,4-triene-3,17-diol
-
Homo sapiens
anastrozole
-
Homo sapiens
estrone-3-sulfamate potent estrone sulfatase inhibitor that causes irreversible inactivation of the enzyme Homo sapiens
letrozole
-
Homo sapiens
additional information sulfamoyloxy-substituted 2-phenylindoles are developed as antiestrogen-based inhibitors of estrone sulfatase. A series of compounds that can inhibit both aromatase and sulfatase is developed based on the structure of estrone 3-sulfamate, a typical estrone sulfatase inhibitor; synthesis and in vitro evaluation of the inhibitory potency of an extended series of 17alpha derivatives of estradiol, structure-activity relationship study, overview Homo sapiens
STX64 i.e. 667 Coumate or BN83495 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
estrone sulfate + H2O Homo sapiens
-
estrone + sulfate
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast
-
Homo sapiens
-
breast carcinoma cell reduced enzyme activity Homo sapiens
-
liver
-
Homo sapiens
-
placenta
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
estrone sulfatase
-
Homo sapiens
steroid sulfatase
-
Homo sapiens
STS
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
placental microsomes, pH not specified in the publication, temperature not specified in the publication Homo sapiens STX64

General Information

General Information Comment Organism
malfunction hormone-dependent breast cancer might be effectively treated by dual inhibition of aromatase and steroid sulfatase Homo sapiens
additional information active site residues are D35, D36, FGS75, R79, K134, H136, H290, D342, Q343, and K368 Homo sapiens
physiological function steroid sulfatase controls the levels of 3-hydroxysteroids available from circulating steroid sulfates in several normal and malignant tissues Homo sapiens