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Literature summary extracted from

  • Walter, G.; Liebl, R.; von Angerer, E.
    2-Phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells (2004), J. Steroid Biochem. Mol. Biol., 88, 409-420.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.1.6.2 medicine 2-phenylindole sulfamates with antiproliferative activity in breast cancer cells are devoid of estrogenic activity and have the potential for in vivo application as steroid sulfatase inhibitors in the treatment of hormone-dependent breast cancer Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.6.2 2-phenylindole sulfamate 2-phenylindole sulfamates with lipophilic side chains in 1- or 5-position of the indole with IC50-values between 2 nM and 0.001 mM, irreversibly inhibits hydrolysis of estrone sulfate in MDA-MB 231 cells, inhibits gene activation in estrogen receptor-positive MCF-7 breast cancer cells in submicromolar concentrations and reduces cell proliferation with IC50 of 0.001 mM Homo sapiens
3.1.6.2 estrone-3-O-sulfamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.1.6.2 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.6.2 MCF-7/2a cell stably transfected breast cancer cells Homo sapiens
-
3.1.6.2 MDA-MB-231 cell mammary carcinoma cell line Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.6.2 estrone sulfate + H2O
-
 Homo sapiens estrone + sulfate
-
 ?
3.1.6.2 estrone sulfate + H2O natural substrate Homo sapiens estrone + sulfate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.6.2 estrone sulfatase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.6.2 0.001
-
 2-phenylindole sulfamates with lipophilic side chains in 1- or 5-position of the indole with IC50-values between 2 nM and 0.001 mM, irreversibly inhibits hydrolysis of estrone sulfate in MDA-MB 231 cells, inhibits gene activation in estrogen receptor-posi Homo sapiens 2-phenylindole sulfamate