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Literature summary extracted from
- Identification of a tumor-promoter cholesterol metabolite in human breast cancers acting through the glucocorticoid receptor (2017), Proc. Natl. Acad. Sci. USA, 114, E9346-E9355.
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 1.1.1.146 | medicine | in breast cancer tissue, cholesterol epoxide hydrolase ChEH metabolizes cholesterol-5,6-epoxide into cholestane-3beta,5alpha,6beta-triol, which is transformed into the oncometabolite 6-oxo-cholestan-3beta,5alpha-diol by 11beta-hydroxysteroid-dehydrogenase 11betaHSD2. ChEH inhibition and 11betaHSD2 silencing inhibit 6-oxo-cholestan-3beta,5alpha-diol production and tumor growth. Patient breast cancer samples show significantly increased 6-oxocholestan-3beta,5alpha-diol levels and greater ChEH and 11betaHSD2 protein expression compared with normal tissues, and 11betaHSD2 and ChEH overexpression correlate with a higher risk of patient death | Homo sapiens |
| 3.3.2.11 | medicine | in breast cancer tissue, cholesterol epoxide hydrolase ChEH metabolizes cholesterol-5,6-epoxide into cholestane-3beta,5alpha,6beta-triol, which is transformed into the oncometabolite 6-oxo-cholestan-3beta,5alpha-diol by 11beta-hydroxysteroid-dehydrogenase 11betaHSD2. ChEH inhibition and 11betaHSD2 silencing inhibit 6-oxo-cholestan-3beta,5alpha-diol production and tumor growth. Patient breast cancer samples show significantly increased 6-oxocholestan-3beta,5alpha-diol levels and greater ChEH and 11betaHSD2 protein expression compared with normal tissues, and 11betaHSD2 and ChEH overexpression correlate with a higher risk of patient death | Homo sapiens |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 1.1.1.146 | - |
Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.3.2.11 | 1-[2-[4-(phenylmethyl)phenoxy]ethyl]-pyrrolidine | - |
Homo sapiens |  |
| 3.3.2.11 | 4-hydroxytamoxifen | - |
Homo sapiens | |
| 3.3.2.11 | clomiphene | - |
Homo sapiens | |
| 3.3.2.11 | dendrogenin A | - |
Homo sapiens | |
| 3.3.2.11 | raloxifene | - |
Homo sapiens | |
| 3.3.2.11 | rimcazole | - |
Homo sapiens | |
| 3.3.2.11 | tamoxifen | - |
Homo sapiens | |
| 3.3.2.11 | tesmilifene | - |
Homo sapiens | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 1.1.1.146 | Homo sapiens | P80365 | - |
- |
| 3.3.2.11 | Homo sapiens | - |
- |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 1.1.1.146 | MCF-7 cell | - |
Homo sapiens | - |
| 1.1.1.146 | MDA-MB-231 cell | - |
Homo sapiens | - |
| 3.3.2.11 | MCF-7 cell | - |
Homo sapiens | - |
| 3.3.2.11 | MDA-MB-231 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 1.1.1.146 | cholestane-3beta,5alpha,6beta-triol + NAD(P)+ | - |
Homo sapiens | 6-oxocholestan-3beta,5alpha-diol + NAD(P)H + H+ | - |
? | |
| 3.3.2.11 | 5,6alpha-epoxy-5alpha-cholestan-3beta-ol + H2O | - |
Homo sapiens | cholestane-3beta,5alpha,6beta-triol | - |
? | |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.3.2.11 | 0.00006 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | clomiphene | |
| 3.3.2.11 | 0.000064 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | clomiphene | |
| 3.3.2.11 | 0.000065 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-hydroxytamoxifen | |
| 3.3.2.11 | 0.000069 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | raloxifene | |
| 3.3.2.11 | 0.00007 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | tamoxifen | |
| 3.3.2.11 | 0.000095 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 4-hydroxytamoxifen | |
| 3.3.2.11 | 0.0001 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | raloxifene | |
| 3.3.2.11 | 0.00011 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | tamoxifen | |
| 3.3.2.11 | 0.000172 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | tesmilifene | |
| 3.3.2.11 | 0.00021 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | tesmilifene | |
| 3.3.2.11 | 0.000231 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[2-[4-(phenylmethyl)phenoxy]ethyl]-pyrrolidine | |
| 3.3.2.11 | 0.00025 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[2-[4-(phenylmethyl)phenoxy]ethyl]-pyrrolidine | |
| 3.3.2.11 | 0.000313 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | dendrogenin A | |
| 3.3.2.11 | 0.00035 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | dendrogenin A | |
| 3.3.2.11 | 0.003 | - |
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | rimcazole | |
| 3.3.2.11 | 0.0035 | - |
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | rimcazole | |
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