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Literature summary for 1.1.1.213 extracted from

  • Steckelbroeck, S.; Oyesanmi, B.; Jin, Y.; Lee, S.H.; Kloosterboer, H.J.; Penning, T.M.
    Tibolone metabolism in human liver is catalyzed by 3alpha/3beta-hydroxysteroid dehydrogenase activities of the four isoforms of the aldo-keto reductase (AKR)1C subfamily (2006), J. Pharmacol. Exp. Ther., 316, 1300-1309.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
Flufenamic acid a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM Homo sapiens
additional information no inhibition by the bile acid 5beta-cholanic acid-3alpha,7alpha-diol Homo sapiens
Phenolphthalein AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-
additional information subcellular localization study, overview Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
tibolone + NADPH + H+ Homo sapiens tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer 3-hydroxytibolone + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
hepatocyte primary, high expression and activity in healthy hepatocytes Homo sapiens
-
liver high expression and activity in female and male liver Homo sapiens
-
additional information no activity in the hepatoma cell line Hep-G2 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
tibolone + NADPH + H+ tibolone is used to treat climacteric symptoms and prevent osteoporosis, it exerts tissue-selective effects via site-specific metabolism into 3alpha- and 3beta-hydroxymetabolites and a DELTA4-isomer Homo sapiens 3-hydroxytibolone + NADP+
-
?
tibolone + NADPH + H+ i.e. [7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one, stereoselctive reaction to the 3alpha-hydroxytibolone product Homo sapiens 3-hydroxytibolone + NADP+
-
?

Synonyms

Synonyms Comment Organism
AKR1C4
-
Homo sapiens
More cf. EC 1.1.1.50, the enzyme belongs to the aldo-keto reductase subfamily AKR1C Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
AKR1C4-selective inhibitor, in vitro and in vivo inhibition, IC50: 0.0004 mM Homo sapiens Phenolphthalein
1.084
-
a nonsteroidalanti-inflammatory drug, IC50: 1.084 mM Homo sapiens Flufenamic acid