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Literature summary for 3.3.2.11 extracted from

  • Voisin, M.; de Medina, P.; Mallinger, A.; Dalenc, F.; Huc-Claustre, E.; et, al.
    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.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
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

Inhibitors

Inhibitors Comment Organism Structure
1-[2-[4-(phenylmethyl)phenoxy]ethyl]-pyrrolidine
-
Homo sapiens
4-hydroxytamoxifen
-
Homo sapiens
clomiphene
-
Homo sapiens
dendrogenin A
-
Homo sapiens
raloxifene
-
Homo sapiens
rimcazole
-
Homo sapiens
tamoxifen
-
Homo sapiens
tesmilifene
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,6alpha-epoxy-5alpha-cholestan-3beta-ol + H2O
-
Homo sapiens cholestane-3beta,5alpha,6beta-triol
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens clomiphene
0.000064
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens clomiphene
0.000065
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-hydroxytamoxifen
0.000069
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens raloxifene
0.00007
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens tamoxifen
0.000095
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-hydroxytamoxifen
0.0001
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens raloxifene
0.00011
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens tamoxifen
0.000172
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens tesmilifene
0.00021
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens tesmilifene
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
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
0.000313
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens dendrogenin A
0.00035
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens dendrogenin A
0.003
-
MCF-7 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens rimcazole
0.0035
-
MDA-MB231 cells, pH not specified in the publication, temperature not specified in the publication Homo sapiens rimcazole