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Literature summary for 1.1.1.270 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

Cloned(Commentary)

Cloned (Comment) Organism
quantitative expression analysis of AKR1C isozymes Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5beta-cholanic acid-3alpha,7alpha-diol
-
Homo sapiens
Flufenamic acid in vitro and in vivo inhibition of AKR1C1 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
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Homo sapiens 5829
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information 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, In Hep-G2 cell cytosol and intact cells tibolone is exclusively reduced to 3beta-hydroxytibolone, 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, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
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isozymes AKR1C1 and AKR1C2
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Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
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Homo sapiens
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hepatocyte primary, time-dependent reduction of tibolone into 3beta- and 3alpha-hydroxytibolone was observed again in a 4:1 ratio Homo sapiens
-
liver
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Homo sapiens
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information 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, In Hep-G2 cell cytosol and intact cells tibolone is exclusively reduced to 3beta-hydroxytibolone, 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, overview Homo sapiens ?
-
?
additional information comparison of substrate specificity and enantioselectivity of AKR1C isozymes, overview Homo sapiens ?
-
?
[7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one + NADPH i.e. tibolone, a synthetic hormone Homo sapiens [7alpha,17alpha]-17-hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-ol + NADP+ reaction product determination and analysis ?

Synonyms

Synonyms Comment Organism
3-ketosteroid reductase
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Homo sapiens
3beta-hydroxysteroid dehydrogenase
-
Homo sapiens
AKR1C1
-
Homo sapiens
AKR1C2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens