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Literature summary extracted from

  • Penning, T.M.; Jin, Y.; Heredia, V.V.; Lewis, M.
    Structure-function relationships in 3alpha-hydroxysteroid dehydrogenases: a comparison of the rat and human isoforms (2003), J. Steroid Biochem. Mol. Biol., 85, 247-255.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.50 expression of isozyme AKR1C2 in Escherichia coli Homo sapiens
1.1.1.50 expression of wild-type and mutant enzymes in Escherichia coli Rattus norvegicus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.50 recombinant type 3 isozyme AKR1C2 in complex with NADP+ and ursodeoxycholate, X-ray structure determination and analysis at 3.0 A resolution Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
1.1.1.50 F118A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 L54A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 N306A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 T226A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 T24A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 W227A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus
1.1.1.50 Y310A site-directed mutagenesis, altered kinetic and catalytic efficiency compared to the wild-type enzyme Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.50 ursodeoxycholate
-
 Homo sapiens
1.1.1.50 ursodeoxycholate
-
 Rattus norvegicus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.1.1.50 additional information
-
 additional information kinetic mechanism, substrate binding mechanism of isozyme AKR1C2 Homo sapiens
1.1.1.50 additional information
-
 additional information kinetic mechanism, substrate binding mechanism of isozyme AKR1C9, wild-type and mutant enzymes Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.1.1.50 additional information Rattus norvegicus enzyme inactivates steroid hormones in the liver, regulates 5alpha-dihydrotestosterone levels in the prostate, and forms the neurosteroid allopregnanolone in the CNS ?
-
 ?
1.1.1.50 additional information Homo sapiens enzyme inactivates steroid hormones in the liver, regulates 5alpha-dihydrotestosterone levels in the prostate, and forms the neurosteroid allopregnanolone in the CNS, isozymes might be involved in regulation of the levels of active androgens, estrogens, and progestrins ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.50 Homo sapiens
-
 4 isozyme AKR1C1-AKR1C4
-
1.1.1.50 Rattus norvegicus
-
 isozyme AKR1C9
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.50 recombinant wild-type and mutant enzymes from Escherichia coli Rattus norvegicus

Reaction

EC Number Reaction Comment Organism Reaction ID
1.1.1.50 a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ isozymes also performs 17- and 20-ketosteroid reductase and 3alpha-, 17beta- and 20alpha-hydroxysteroid oxidase activities at varying rates Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.50 brain
-
 Homo sapiens
-
1.1.1.50 brain
-
 Rattus norvegicus
-
1.1.1.50 Hep-G2 cell isozyme AKR1C2 Homo sapiens
-
1.1.1.50 liver
-
 Homo sapiens
-
1.1.1.50 liver
-
 Rattus norvegicus
-
1.1.1.50 additional information tissue-specific distribution of the different isozymes Homo sapiens
-
1.1.1.50 prostate
-
 Homo sapiens
-
1.1.1.50 prostate
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.1.1.50 additional information
-
 isozyme AKR1C9 Rattus norvegicus
1.1.1.50 additional information
-
 isozymes AKR1C1-AKR1C4 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+
-
 Rattus norvegicus 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 ?
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ type 2 isozyme AKR1C3 catalyzes the forward reaction, type 3 isozyme AKR1C2 catalyzes the reverse reaction Homo sapiens 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 ir
1.1.1.50 5alpha-dihydroprogesterone + NADPH + H+ type 3 isozyme AKR1C2 Homo sapiens 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 r
1.1.1.50 additional information structure-function relationship Homo sapiens ?
-
 ?
1.1.1.50 additional information enzyme inactivates steroid hormones in the liver, regulates 5alpha-dihydrotestosterone levels in the prostate, and forms the neurosteroid allopregnanolone in the CNS Rattus norvegicus ?
-
 ?
1.1.1.50 additional information enzyme inactivates steroid hormones in the liver, regulates 5alpha-dihydrotestosterone levels in the prostate, and forms the neurosteroid allopregnanolone in the CNS, isozymes might be involved in regulation of the levels of active androgens, estrogens, and progestrins Homo sapiens ?
-
 ?
1.1.1.50 additional information enzyme acts positional and stereospecific, structure-function relationship Rattus norvegicus ?
-
 ?
1.1.1.50 testosterone + NADPH + H+
-
 Homo sapiens ?
-
 ?
1.1.1.50 testosterone + NADPH + H+ residues involved in substrate binding are T24, L54, F118, T226, W227, N306, and Y310 Rattus norvegicus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.50 3alpha-HSD
-
 Homo sapiens
1.1.1.50 3alpha-HSD
-
 Rattus norvegicus
1.1.1.50 3alpha-hydroxysteroid dehydrogenase
-
 Homo sapiens
1.1.1.50 3alpha-hydroxysteroid dehydrogenase
-
 Rattus norvegicus
1.1.1.50 More enzyme belongs to the aldo-keto reductase superfamily Rattus norvegicus
1.1.1.50 More enzymes belongs to the aldo-keto reductase superfamily Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.50 NADP+ binding to isozyme AKR1C2, mechanism and structure Homo sapiens