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