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Literature summary extracted from

  • Skarydova, L.; Zivna, L.; Xiong, G.; Maser, E.; Wsol, V.
    AKR1C3 as a potential target for the inhibitory effect of dietary flavonoids (2009), Chem. Biol. Interact., 178, 138-144.
    View publication on PubMed

Application

EC Number Application Comment Organism
1.1.1.213 drug development 2'-hydroxyflavanone may be useful for clinical therapy of malignancies where AKR1C3 is overexpressed like in prostate and breast cancer Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.213 AKR1C3 PCR fragment cloned into pCR2.1-TOPO and then into vector pET15b and overexpressed in Escherichia coli strain BL21(DE3) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.213 2'-hydroxyflavanone most potent inhibitor, 0.02 mM inhibits by 98.9% and in an uncompetitive manner Homo sapiens
1.1.1.213 3-hydroxyflavone
-
 Homo sapiens
1.1.1.213 4'-hydroxyflavanone
-
 Homo sapiens
1.1.1.213 5-hydroxyflavone
-
 Homo sapiens
1.1.1.213 7-hydroxyflavone very potent inhibitor, 0.02 mM inhibits by 82.5% Homo sapiens
1.1.1.213 apigenin 0.02 mM inhibits by ca. 50% Homo sapiens
1.1.1.213 chlorogenic acid
-
 Homo sapiens
1.1.1.213 epigallocatechin gallate
-
 Homo sapiens
1.1.1.213 isovitexin
-
 Homo sapiens
1.1.1.213 luteolin 0.02 mM inhibits by ca. 50% Homo sapiens
1.1.1.213 additional information is not inhibited by 0.02 mM caffeic acid, rutin, 4-hydroxybenzoic acid, cyanin chloride and taxifolin Homo sapiens
1.1.1.213 naringenin very potent inhibitor, 0.02 mM inhibits by 71.9% Homo sapiens
1.1.1.213 quercetin 0.02 mM inhibits by ca. 50% Homo sapiens
1.1.1.213 silibinin 0.02 mM inhibits by ca. 50% Homo sapiens
1.1.1.213 vitexin
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.213 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.213 oracin + NADPH
-
 Homo sapiens ? + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.213 17beta-hydroxysteroid dehydrogenase type 5
-
 Homo sapiens
1.1.1.213 3alpha-hydroxysteroid dehydrogenase type 2
-
 Homo sapiens
1.1.1.213 AKR1C3
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.213 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.213 0.0003
-
-
 Homo sapiens 2'-hydroxyflavanone
1.1.1.213 0.0024
-
-
 Homo sapiens naringenin
1.1.1.213 0.0049
-
-
 Homo sapiens 7-hydroxyflavone
1.1.1.213 0.0062
-
-
 Homo sapiens silibinin
1.1.1.213 0.0188
-
-
 Homo sapiens quercetin
1.1.1.213 0.0218
-
-
 Homo sapiens apigenin
1.1.1.213 0.0374
-
-
 Homo sapiens luteolin