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Literature summary for 1.1.1.209 extracted from

  • Dhagat, U.; Endo, S.; Mamiya, H.; Hara, A.; El-Kabbani, O.
    Studies on a Tyr residue critical for the binding of coenzyme and substrate in mouse 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21): structure of the Y224D mutant enzyme (2010), Acta Crystallogr. Sect. D, 66, 198-204.
    View publication on PubMed
Search for more literature for 1.1.1.209

Crystallization (Commentary)

Crystallization (Comment) Organism
Y224D mutant at 2.3 A resolution. Mutation results in a change in the conformation of the flexible loop B, including the V-shaped groove Mus musculus

Protein Variants

Protein Variants Comment Organism
Q222N mutation of residue involved in forming the safety belt for binding of the coenzyme. Kinetic constants for 3-hydroxy/3-ketosteroids and 17-hydroxy/ketosteroids similar to wild type Mus musculus
Y224D mutation reduces the Km value for NADP(H) by up to 80fold and completely reverses the 17alpha stereospecificity of the enzyme Mus musculus
Y224F mutation of residue involved in forming the safety belt for binding of the coenzyme. Kinetic constants for 3-hydroxy/3-ketosteroids and 17-hydroxy/ketosteroids similar to wild type Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0001
-
 lithocholic acid wild-type, pH 7.0, 25°C Mus musculus
0.0002
-
 4-androstene-3,17-dione wild-type, pH 7.0, 25°C Mus musculus
0.0002
-
 5beta-pregnane-20alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
0.0002
-
 lithocholic acid mutant Y224F, pH 7.0, 25°C Mus musculus
0.0004
-
 5alpha-Androstan-17alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
0.0004
-
 5beta-pregnane-3,20-dione mutant Q222N, pH 7.0, 25°C Mus musculus
0.0005
-
 5beta-pregnane-3,20-dione mutant Y224F, pH 7.0, 25°C Mus musculus
0.0006
-
 5beta-pregnane-3,20-dione wild-type, pH 7.0, 25°C Mus musculus
0.0006
-
 Epitestosterone wild-type, pH 7.0, 25°C Mus musculus
0.0006
-
 5alpha-Androstan-3alpha-ol-17-one wild-type, pH 7.0, 25°C Mus musculus
0.0006
-
 5beta-pregnane-3alpha,20alpha-diol wild-type, pH 7.0, 25°C Mus musculus
0.0006
-
 lithocholic acid mutant Q222N, pH 7.0, 25°C Mus musculus
0.0006
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.0007
-
 5beta-pregnane-20alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.0015
-
 4-androstene-3,17-dione mutant Y224F, pH 7.0, 25°C Mus musculus
0.0018
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.0032
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224F, pH 7.0, 25°C Mus musculus
0.0034
-
 5alpha-Androstan-3alpha-ol-17-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.0038
-
 5beta-pregnane-3alpha,20alpha-diol mutant Q222N, pH 7.0, 25°C Mus musculus
0.0047
-
 5alpha-androstan-17beta-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.0054
-
 5alpha-Androstan-17alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.0059
-
 4-androstene-3,17-dione mutant Q222N, pH 7.0, 25°C Mus musculus
0.0059
-
 5beta-pregnane-3,20-dione mutant Y224D, pH 7.0, 25°C Mus musculus
0.0067
-
 lithocholic acid mutant Y224D, pH 7.0, 25°C Mus musculus
0.0078
-
 4-androstene-3,17-dione mutant Y224D, pH 7.0, 25°C Mus musculus
0.013
-
 5alpha-androstan-3beta,17beta-diol mutant Y224F, pH 7.0, 25°C Mus musculus
0.014
-
 5alpha-Androstan-17alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.014
-
 Epitestosterone mutant Y224F, pH 7.0, 25°C Mus musculus
0.015
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.015
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.018
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224D, pH 7.0, 25°C Mus musculus
0.02
-
 Epitestosterone mutant Q222N, pH 7.0, 25°C Mus musculus
0.035
-
 5alpha-androstan-3beta,17beta-diol mutant Y224D, pH 7.0, 25°C Mus musculus
0.08
-
 5alpha-androstan-17beta-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.096
-
 5alpha-androstan-17beta-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.1
-
 5alpha-androstan-3beta,17beta-diol mutant Q222N, pH 7.0, 25°C Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus Q91WR5
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-androstene-3,17-dione + NADPH + H+
-
 Mus musculus ? + NADP+
-
 r
5-androstene-3beta,17beta-diol + NADP+ no substrate for wild-type, but substrate for mutants Y224F, Y224D, Q222D Mus musculus ? + NADPH
-
 ?
5alpha-androstan-17alpha-ol-3-one + NADP+
-
 Mus musculus 5alpha-androstan-3,17-dione + NADPH + H+
-
 ?
5alpha-androstan-17beta-ol-3-one + NADP+
-
 Mus musculus 5alpha-androstan-3,17-dione + NADPH + H+ no substrate for wild-type, but substrate for mutants Y224F, Y224D, Q222D ?
5alpha-androstan-3alpha-ol-17-one + NADPH + H+
-
 Mus musculus 5alpha-androstan-3alpha-ol-17beta-ol + NADP+
-
 ?
5alpha-androstan-3beta,17beta-diol + NADP+
-
 Mus musculus ? + NADPH
-
 ?
5alpha-androstan-3beta,17beta-diol + NADP+
-
 Mus musculus ? + NADPH + H+
-
 ?
5beta-pregnane-20alpha-ol-3-one + NADP+
-
 Mus musculus 5beta-pregnane-3alpha,20alpha-diol + NADPH + H+
-
 r
5beta-pregnane-3,20-dione + NADPH + H+
-
 Mus musculus 5beta-pregnane-3alpha-ol-20-one + NADP+
-
 r
5beta-pregnane-3alpha,20alpha-diol + NADPH + H+
-
 Mus musculus 5beta-pregnane-20alpha-ol-3-one + NADP+
-
 r
epitestosterone + NADP+
-
 Mus musculus testosterone + NADPH + H+
-
 ?
lithocholic acid + NADP+
-
 Mus musculus ? + NADPH + H+
-
 r

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.00167
-
 5alpha-androstan-3beta,17beta-diol mutant Y224D, pH 7.0, 25°C Mus musculus
0.00217
-
 5alpha-androstan-3beta,17beta-diol mutant Y224F, pH 7.0, 25°C Mus musculus
0.0025
-
 5alpha-androstan-17beta-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.0027
-
 5alpha-androstan-17beta-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.00367
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224D, pH 7.0, 25°C Mus musculus
0.0073
-
 lithocholic acid mutant Y224D, pH 7.0, 25°C Mus musculus
0.0217
-
 4-androstene-3,17-dione mutant Y224D, pH 7.0, 25°C Mus musculus
0.0217
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.0367
-
 5alpha-androstan-17beta-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.047
-
 lithocholic acid wild-type, pH 7.0, 25°C Mus musculus
0.065
-
 5alpha-androstan-3beta,17beta-diol mutant Q222N, pH 7.0, 25°C Mus musculus
0.073
-
 5alpha-Androstan-3alpha-ol-17-one wild-type, pH 7.0, 25°C Mus musculus
0.081
-
 lithocholic acid mutant Y224F, pH 7.0, 25°C Mus musculus
0.105
-
 lithocholic acid mutant Q222N, pH 7.0, 25°C Mus musculus
0.127
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.167
-
 4-androstene-3,17-dione wild-type, pH 7.0, 25°C Mus musculus
0.167
-
 5alpha-androstan-17beta-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
0.167
-
 5alpha-Androstan-17alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
0.167
-
 5alpha-androstan-3beta,17beta-diol wild-type, pH 7.0, 25°C Mus musculus
0.217
-
 5beta-pregnane-3alpha,20alpha-diol wild-type, pH 7.0, 25°C Mus musculus
0.23
-
 Epitestosterone mutant Q222N, pH 7.0, 25°C Mus musculus
0.233
-
 5alpha-Androstan-3alpha-ol-17-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.25
-
 5beta-pregnane-3alpha,20alpha-diol mutant Q222N, pH 7.0, 25°C Mus musculus
0.283
-
 5alpha-Androstan-17alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
0.3
-
 Epitestosterone wild-type, pH 7.0, 25°C Mus musculus
0.317
-
 4-androstene-3,17-dione mutant Y224F, pH 7.0, 25°C Mus musculus
0.35
-
 5beta-pregnane-3,20-dione mutant Y224D, pH 7.0, 25°C Mus musculus
0.383
-
 5beta-pregnane-20alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
0.4
-
 5beta-pregnane-3,20-dione wild-type, pH 7.0, 25°C Mus musculus
0.4
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224F, pH 7.0, 25°C Mus musculus
0.57
-
 Epitestosterone mutant Y224F, pH 7.0, 25°C Mus musculus
0.617
-
 4-androstene-3,17-dione mutant Q222N, pH 7.0, 25°C Mus musculus
0.867
-
 5alpha-Androstan-17alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
1.25
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
2.83
-
 5beta-pregnane-20alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
4
-
 5beta-pregnane-3,20-dione mutant Y224F, pH 7.0, 25°C Mus musculus
4.83
-
 5beta-pregnane-3,20-dione mutant Q222N, pH 7.0, 25°C Mus musculus
4.83
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.03
-
 5alpha-androstan-17beta-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
0.05
-
 5alpha-androstan-3beta,17beta-diol mutant Y224D, pH 7.0, 25°C Mus musculus
0.167
-
 5alpha-androstan-3beta,17beta-diol mutant Y224F, pH 7.0, 25°C Mus musculus
0.5
-
 5alpha-androstan-17beta-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
0.65
-
 5alpha-androstan-3beta,17beta-diol mutant Q222N, pH 7.0, 25°C Mus musculus
1
-
 lithocholic acid mutant Y224D, pH 7.0, 25°C Mus musculus
1
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224D, pH 7.0, 25°C Mus musculus
1.5
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224D, pH 7.0, 25°C Mus musculus
3.3
-
 4-androstene-3,17-dione mutant Y224D, pH 7.0, 25°C Mus musculus
4.5
-
 5alpha-androstan-17beta-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
11.67
-
 Epitestosterone mutant Q222N, pH 7.0, 25°C Mus musculus
20
-
 5alpha-Androstan-17alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
40
-
 Epitestosterone mutant Y224F, pH 7.0, 25°C Mus musculus
60
-
 5beta-pregnane-3,20-dione mutant Y224D, pH 7.0, 25°C Mus musculus
65
-
 5beta-pregnane-3alpha,20alpha-diol mutant Q222N, pH 7.0, 25°C Mus musculus
68.3
-
 5alpha-Androstan-3alpha-ol-17-one mutant Q222N, pH 7.0, 25°C Mus musculus
70
-
 5alpha-Androstan-3alpha-ol-17-one mutant Y224F, pH 7.0, 25°C Mus musculus
83
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224D, pH 7.0, 25°C Mus musculus
105
-
 4-androstene-3,17-dione mutant Q222N, pH 7.0, 25°C Mus musculus
122
-
 5alpha-Androstan-3alpha-ol-17-one wild-type, pH 7.0, 25°C Mus musculus
125
-
 5beta-pregnane-3alpha,20alpha-diol mutant Y224F, pH 7.0, 25°C Mus musculus
160
-
 5alpha-Androstan-17alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus
183
-
 lithocholic acid mutant Q222N, pH 7.0, 25°C Mus musculus
217
-
 4-androstene-3,17-dione mutant Y224F, pH 7.0, 25°C Mus musculus
366
-
 5beta-pregnane-3alpha,20alpha-diol wild-type, pH 7.0, 25°C Mus musculus
400
-
 5beta-pregnane-20alpha-ol-3-one mutant Q222N, pH 7.0, 25°C Mus musculus
400
-
 lithocholic acid mutant Y224F, pH 7.0, 25°C Mus musculus
417
-
 5alpha-Androstan-17alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
467
-
 lithocholic acid wild-type, pH 7.0, 25°C Mus musculus
500
-
 Epitestosterone wild-type, pH 7.0, 25°C Mus musculus
667
-
 5beta-pregnane-3,20-dione wild-type, pH 7.0, 25°C Mus musculus
833
-
 4-androstene-3,17-dione wild-type, pH 7.0, 25°C Mus musculus
1200
-
 5beta-pregnane-3,20-dione mutant Q222N, pH 7.0, 25°C Mus musculus
2000
-
 5beta-pregnane-20alpha-ol-3-one wild-type, pH 7.0, 25°C Mus musculus
8000
-
 5beta-pregnane-3,20-dione mutant Y224F, pH 7.0, 25°C Mus musculus
8000
-
 5beta-pregnane-20alpha-ol-3-one mutant Y224F, pH 7.0, 25°C Mus musculus