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Literature summary for 1.1.1.64 extracted from

  • Brozic, P.; Golob, B.; Gomboc, N.; Rizner, T.L.; Gobec, S.
    Cinnamic acids as new inhibitors of 17beta-hydroxysteroid dehydrogenase type 5 (AKR1C3) (2006), Mol. Cell. Endocrinol., 248, 233-235.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of AKR1C3 in Eschericha coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-methylcinnamic acid IC50: 0.0064 mM Homo sapiens
3,4,5-trimethoxycinnamic acid IC50: 0.049 mM Homo sapiens
3-coumaric acid 34% inhibition at 0.05 mM Homo sapiens
3-cyclohexylpropanoic acid weak inhibition, IC50: 0.1 mM, above Homo sapiens
3-trifluoromethylcinnamic acid IC50: 0.043 mM Homo sapiens
caffeic acid 18% inhibition at 0.05 mM Homo sapiens
Cinnamic acid IC50: 0.050 mM Homo sapiens
coumarin-3-carboxylic acid 30% inhibition at 0.05 mM Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
androst-4-ene-3,17-dione + NADPH Homo sapiens convertion of the weak androgen androstendione into the potent androgen testosterone testosterone + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
9,10-phenanthrenequinone + NADPH
-
Homo sapiens ?
-
?
androst-4-ene-3,17-dione + NADPH
-
Homo sapiens testosterone + NADP+
-
?
androst-4-ene-3,17-dione + NADPH convertion of the weak androgen androstendione into the potent androgen testosterone Homo sapiens testosterone + NADP+
-
?

Synonyms

Synonyms Comment Organism
17beta-HSD type 5
-
Homo sapiens
17beta-hydroxysteroid dehydrogenase type 5
-
Homo sapiens
AKR1C3
-
Homo sapiens
More the enzyme belongs to the aldo-keto reductase family Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0064
-
IC50: 0.0064 mM Homo sapiens 2-methylcinnamic acid
0.043
-
IC50: 0.043 mM Homo sapiens 3-trifluoromethylcinnamic acid
0.049
-
IC50: 0.049 mM Homo sapiens 3,4,5-trimethoxycinnamic acid
0.05
-
IC50: 0.050 mM Homo sapiens Cinnamic acid
0.1
-
weak inhibition, IC50: 0.1 mM, above Homo sapiens 3-cyclohexylpropanoic acid