Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 1.1.1.62 extracted from

  • Sali, V.K.; Mani, S.; Meenaloshani, G.; Velmurugan Ilavarasi, A.; Vasanthi, H.R.
    Type 5 17-hydroxysteroid dehydrogenase/prostaglandin F synthase (AKR1C3) inhibition and potential anti-proliferative activity of cholest-4-ene-3,6-dione in MCF-7 breast cancer cells (2020), Steroids, 159, 108638 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
cholest-4-ene-3,6-dione cholest-4-ene-3,6-dione arrests the enzymatic conversion of estrone to 17-beta estradiol, by inhibiting AKR1C3 in intact MCF-7 cells. It can be used as a molecular scaffold for further development of l small-molecules with better specificity towards AKR1C3; the inhibitor occupies the binding region of AKR1C3 with almost similar orientation as indomethacin, thereby acting as an antagonistic agent for AKR1C3. It induces inhibition of AKR1C3 and cell death in MCF-7 cells. IT can be used as a molecular scaffold for development of novel small-molecules with better specificity towards AKR1C3 Homo sapiens
indomethacin specific inhibitor for AKR1C3 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
estrone + NADPH + H+ Homo sapiens
-
17beta-estradiol + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens P42330
-
-

Source Tissue

Source Tissue Comment Organism Textmining
MCF-7 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
estrone + NADPH + H+
-
Homo sapiens 17beta-estradiol + NADP+
-
?

Synonyms

Synonyms Comment Organism
AKR1C3
-
Homo sapiens
type 5 17-hydroxysteroid dehydrogenase/prostaglandin F synthase
-
Homo sapiens