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

BRENDA support

Literature summary for 1.1.1.213 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

Application Comment Organism
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)

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

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