Crystallization (Comment) | Organism |
---|---|
crystal structure analysis of placenta microsome enzyme, overview | Homo sapiens |
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 | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
estrone sulfate + H2O | Homo sapiens | - |
estrone + sulfate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
breast | - |
Homo sapiens | - |
breast carcinoma cell | reduced enzyme activity | Homo sapiens | - |
liver | - |
Homo sapiens | - |
placenta | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
estrone sulfate + H2O | - |
Homo sapiens | estrone + sulfate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
estrone sulfatase | - |
Homo sapiens |
steroid sulfatase | - |
Homo sapiens |
STS | - |
Homo sapiens |
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 | 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 |