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Literature summary for 1.1.1.50 extracted from

  • Jin, Y.; Cooper, W.C.; Penning, T.M.
    Examination of the differences in structure-function of human and rat 3alpha-hydroxysteroid dehydrogenase (2003), Chem. Biol. Interact., 143-144, 383-392.
    View publication on PubMed

Application

Application Comment Organism
medicine enzyme is a potential drug target Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expression of isozymes AKR1C1-4 in Escherichia coli Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
isozyme AKR1C2 in ternary complex with NADP+ and ursodeoxycholate, X-ray diffraction structure determination and analysis at 3.0 A resolution, molecular replacement Homo sapiens
isozyme AKR1C9 in ternary complex with NADP+ and ursodeoxycholate, X-ray diffraction structure determination and analysis at 2.8 A resolution Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information cofactor binding kinetics Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ Homo sapiens isozyme AKR1C4 pregnan-3alpha,20beta-diol + 2 NADP+
-
r
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ Rattus norvegicus isozyme AKR1C9 pregnan-3alpha,20beta-diol + 2 NADP+
-
r
additional information Rattus norvegicus enzyme regulates the occupancy and trans-activation of steroid hormone receptors by interconverting potent hormones with their cognate inactive metabolites ?
-
?
additional information Homo sapiens physiological roles of the isozymes AKR1C1-4, overview, enzyme regulates the occupancy and trans-activation of steroid hormone receptors by interconverting potent hormones with their cognate inactive metabolites ?
-
?

Organism

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

Reaction

Reaction Comment Organism Reaction ID
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ steroid binding pocket structure of isozyme AKR1C2 Homo sapiens
a 3alpha-hydroxysteroid + NAD(P)+ = a 3-oxosteroid + NAD(P)H + H+ steroid binding pocket structure of isozyme AKR1C9 Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
liver isozyme AKR1C4 Homo sapiens
-
prostate isozyme AKR1C4 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
additional information
-
-
Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ isozyme AKR1C4 Homo sapiens pregnan-3alpha,20beta-diol + 2 NADP+
-
r
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ isozyme AKR1C9 Rattus norvegicus pregnan-3alpha,20beta-diol + 2 NADP+
-
r
5alpha-dihydroprogesterone + 2 NADPH + 2 H+ preferred substrate for isozyme AKR1C4, while isozymes AKR1C1-3 show only low activity Homo sapiens pregnan-3alpha,20beta-diol + 2 NADP+
-
r
additional information enzyme regulates the occupancy and trans-activation of steroid hormone receptors by interconverting potent hormones with their cognate inactive metabolites Rattus norvegicus ?
-
?
additional information physiological roles of the isozymes AKR1C1-4, overview, enzyme regulates the occupancy and trans-activation of steroid hormone receptors by interconverting potent hormones with their cognate inactive metabolites Homo sapiens ?
-
?
additional information isozyme is positional- and stereospecific for the 3alpha-hydroxy steroid dehydrogenase reaction Rattus norvegicus ?
-
?
additional information isozymes display 3alpha-, 17beta-, and 20alpha-hydroxysteroid dehydrogenase activities to varying degrees, isozyme AKR1C4 shows the highest 3alpha-hydroxysteroid dehydrogenase activity of all isozymes, overview Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
More isozyme AKR1C2 shows an (alphabeta)8-barrel structure Homo sapiens

Synonyms

Synonyms Comment Organism
3alpha-hydroxysteroid dehydrogenase
-
Homo sapiens
3alpha-hydroxysteroid dehydrogenase
-
Rattus norvegicus
AKR1C1-4
-
Homo sapiens
AKR1C9
-
Rattus norvegicus
HSD
-
Homo sapiens
HSD
-
Rattus norvegicus
More enzyme belongs to the aldo-keto reductase superfamily Homo sapiens
More enzyme belongs to the aldo-keto reductase superfamily Rattus norvegicus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.02
-
5alpha-dihydrotestosterone isozyme AKR1C2 Homo sapiens
1
-
5alpha-dihydrotestosterone isozyme AKR1C9 Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADP+ binding and release mechanism Homo sapiens
NADP+ binding and release mechanism Rattus norvegicus
NADPH binding and release mechanism Homo sapiens
NADPH binding and release mechanism Rattus norvegicus