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Literature summary for 1.1.1.50 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
Search for more literature for 1.1.1.50

Cloned(Commentary)

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

Crystallization (Commentary)

Crystallization (Comment) Organism
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

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

Inhibitors

Inhibitors Comment Organism Structure
ursodeoxycholate
-
 Homo sapiens
ursodeoxycholate
-
 Rattus norvegicus

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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 ?
-
 ?
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

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

Purification (Commentary)

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

Reaction

Reaction Comment Organism Reaction ID
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

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

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5alpha-dihydroprogesterone + NADPH + H+
-
 Rattus norvegicus 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 ?
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
5alpha-dihydroprogesterone + NADPH + H+ type 3 isozyme AKR1C2 Homo sapiens 3alpha,5alpha-3-hydroxypregnan-20-one + NADP+
-
 r
additional information structure-function relationship Homo sapiens ?
-
 ?
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 ?
-
 ?
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 ?
-
 ?
additional information enzyme acts positional and stereospecific, structure-function relationship Rattus norvegicus ?
-
 ?
testosterone + NADPH + H+
-
 Homo sapiens ?
-
 ?
testosterone + NADPH + H+ residues involved in substrate binding are T24, L54, F118, T226, W227, N306, and Y310 Rattus norvegicus ?
-
 ?

Synonyms

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

Cofactor

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