BRENDA - Enzyme Database show
show all sequences of 1.1.1.209

Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors

Dhagat, U.; Endo, S.; Hara, A.; El-Kabbani, O.; Bioorg. Med. Chem. 16, 3245-3254 (2008)

Data extracted from this reference:

Inhibitors
Inhibitors
Commentary
Organism
Structure
chrysin
-
Mus musculus
fidarestat
-
Mus musculus
minalrestat
inhibition pattern for AKR1C21, overview
Mus musculus
additional information
enzyme-inhibitor complexe modelling, Tyr118 and Phe311 are important residues for inhibitor recognition and orientation in the active site of AKR1C21, overview
Mus musculus
myricetin
-
Mus musculus
quercetin
inhibition pattern for AKR1C21, overview
Mus musculus
quercitrin
-
Mus musculus
sorbinil
-
Mus musculus
Tolrestat
inhibition pattern for AKR1C21, overview
Mus musculus
zopolrestat
-
Mus musculus
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
additional information
Mus musculus
the enzyme catalyses the oxidoreduction of steroid hormones such as estrogens, androgens and neurosteroids
?
-
-
-
Organism
Organism
Primary Accession No. (UniProt)
Commentary
Textmining
Mus musculus
-
-
-
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
the enzyme catalyses the oxidoreduction of steroid hormones such as estrogens, androgens and neurosteroids
685538
Mus musculus
?
-
-
-
-
Temperature Optimum [°C]
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
25
-
assay at
Mus musculus
pH Optimum
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.4
-
assay at
Mus musculus
IC50 Value
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000009
-
pH 7.4, 25°C
Mus musculus
fidarestat
0.00003
-
pH 7.4, 25°C
Mus musculus
zopolrestat
0.00004
-
pH 7.4, 25°C
Mus musculus
Tolrestat
0.00007
-
pH 7.4, 25°C
Mus musculus
minalrestat
0.00015
-
pH 7.4, 25°C
Mus musculus
quercitrin
0.00091
-
pH 7.4, 25°C
Mus musculus
sorbinil
0.0022
-
pH 7.4, 25°C
Mus musculus
quercetin
0.0085
-
pH 7.4, 25°C
Mus musculus
chrysin
0.029
-
pH 7.4, 25°C
Mus musculus
myricetin
IC50 Value (protein specific)
IC50 Value
IC50 Value Maximum
Commentary
Organism
Inhibitor
Structure
0.000009
-
pH 7.4, 25°C
Mus musculus
fidarestat
0.00003
-
pH 7.4, 25°C
Mus musculus
zopolrestat
0.00004
-
pH 7.4, 25°C
Mus musculus
Tolrestat
0.00007
-
pH 7.4, 25°C
Mus musculus
minalrestat
0.00015
-
pH 7.4, 25°C
Mus musculus
quercitrin
0.00091
-
pH 7.4, 25°C
Mus musculus
sorbinil
0.0022
-
pH 7.4, 25°C
Mus musculus
quercetin
0.0085
-
pH 7.4, 25°C
Mus musculus
chrysin
0.029
-
pH 7.4, 25°C
Mus musculus
myricetin
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
chrysin
-
Mus musculus
fidarestat
-
Mus musculus
minalrestat
inhibition pattern for AKR1C21, overview
Mus musculus
additional information
enzyme-inhibitor complexe modelling, Tyr118 and Phe311 are important residues for inhibitor recognition and orientation in the active site of AKR1C21, overview
Mus musculus
myricetin
-
Mus musculus
quercetin
inhibition pattern for AKR1C21, overview
Mus musculus
quercitrin
-
Mus musculus
sorbinil
-
Mus musculus
Tolrestat
inhibition pattern for AKR1C21, overview
Mus musculus
zopolrestat
-
Mus musculus
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
additional information
Mus musculus
the enzyme catalyses the oxidoreduction of steroid hormones such as estrogens, androgens and neurosteroids
?
-
-
-
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
additional information
the enzyme catalyses the oxidoreduction of steroid hormones such as estrogens, androgens and neurosteroids
685538
Mus musculus
?
-
-
-
-
Temperature Optimum [°C] (protein specific)
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
25
-
assay at
Mus musculus
pH Optimum (protein specific)
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.4
-
assay at
Mus musculus
Other publictions for EC 1.1.1.209
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
710716
Dhagat
Studies on a Tyr residue criti ...
Mus musculus
Acta Crystallogr. Sect. D
66
198-204
2010
-
-
-
1
3
-
-
36
-
-
-
-
-
2
-
-
-
-
-
-
-
-
12
-
-
-
-
38
-
-
-
-
-
-
-
-
-
-
-
1
3
-
-
-
-
36
-
-
-
-
-
-
-
-
-
-
-
-
12
-
-
-
-
38
-
-
-
-
-
-
-
-
36
36
695325
Dhagat
Structure of the G225P/G226P m ...
Mus musculus
Acta Crystallogr. Sect. D
65
257-265
2009
-
-
1
1
1
-
1
16
-
-
-
-
-
2
-
-
1
-
-
-
-
-
10
-
-
-
-
16
-
-
-
1
-
-
2
-
-
1
1
1
1
-
2
1
-
16
-
-
-
-
-
-
-
1
-
-
-
-
10
-
-
-
-
16
-
-
-
-
-
-
-
-
-
-
685538
Dhagat
Inhibition of 3(17)alpha-hydro ...
Mus musculus
Bioorg. Med. Chem.
16
3245-3254
2008
-
-
-
-
-
-
10
-
-
-
-
1
-
2
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
9
-
-
-
-
-
-
-
9
10
-
-
-
-
-
1
-
-
-
-
-
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
684185
Dhagat
Structure of 3(17)alpha-hydrox ...
Mus musculus
Acta Crystallogr. Sect. F
63
825-830
2007
-
-
-
1
-
-
-
-
-
-
-
3
-
2
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
2
-
-
-
-
-
-
2
1
-
-
-
-
-
-
-
-
-
3
-
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
-
-
-
-
-
667072
El-Kabbani
Crystallization and preliminar ...
Mus musculus
Acta crystallogr. Sect. F
61
688-690
2005
-
-
1
1
-
-
-
-
-
-
1
-
-
2
-
-
1
-
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
1
-
1
-
-
-
-
-
-
-
-
1
-
-
-
-
1
-
1
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
389547
Lin
Expression and characterizatio ...
Homo sapiens
Mol. Endocrinol.
11
1971-1984
1997
-
-
1
-
-
-
-
4
-
-
-
-
-
1
-
-
-
-
-
5
3
-
3
-
-
-
-
4
-
-
-
-
-
-
-
-
-
1
-
-
-
-
-
-
-
4
-
-
-
-
-
-
-
-
-
5
3
-
3
-
-
-
-
4
-
-
-
-
-
-
-
-
-
-
286234
Nakagawa
Identification of two dihydrod ...
Mus musculus
J. Biochem.
106
633-638
1989
-
-
-
-
-
-
10
13
-
-
2
-
-
3
-
-
1
-
-
1
1
-
27
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
10
-
13
-
-
2
-
-
-
-
1
-
1
1
-
27
1
-
-
-
-
1
-
-
-
-
-
-
-
-
-
286232
Lau
A 3(17) alpha-hydroxysteroid d ...
Oryctolagus cuniculus
J. Biol. Chem.
257
9444-9449
1982
-
-
-
-
-
-
-
-
1
-
2
-
-
1
-
-
1
-
-
1
-
1
5
1
-
-
-
-
-
-
-
4
-
-
-
-
-
-
4
-
-
-
-
-
-
-
1
-
2
-
-
-
-
1
-
1
-
1
5
1
-
-
-
-
-
-
-
-
-
-
-
-
-
-
286233
Lau
Comparison of the multiple for ...
Oryctolagus cuniculus
J. Biol. Chem.
257
9450-9456
1982
-
-
-
-
-
-
1
6
1
-
-
-
-
1
-
-
-
-
-
2
-
-
6
-
-
-
-
-
1
-
-
4
-
-
-
-
-
-
4
-
-
-
-
1
-
6
1
-
-
-
-
-
-
-
-
2
-
-
6
-
-
-
-
-
1
-
-
-
-
-
-
-
-
-