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Literature summary for 3.1.6.2 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

Application Comment Organism
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

Inhibitors Comment Organism Structure
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
estrone-3-O-sulfamate
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
estrone sulfatase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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