Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli cells | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
in ternary complex with NADP+ and 3,5-dichlorosalicylic acid, hanging drop vapour diffusion method, using 25% (v/v) polyethylene glycol monomethyl ether 550, 0.02 M zinc sulfate in 0.1 M MES buffer (pH 6.5) | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
H222S | the mutation in AKR1C1 results in a 10fold reduction in the potency of the inhibitor 3,5-dicholorosalicylic acid | Homo sapiens |
L306 | the mutation in AKR1C1 results in a 46fold reduction in the potency of the inhibitor 3,5-dicholorosalicylic acid | Homo sapiens |
L308A | the mutation in AKR1C1 results in a 470fold reduction in the potency of the inhibitor 3,5-dicholorosalicylic acid | Homo sapiens |
L54V | the mutation in AKR1C1 results in a 14fold reduction in the potency of the inhibitor 3,5-dicholorosalicylic acid | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3,5-dichlorosalicylic acid | potent inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q04828 | - |
- |
Purification (Comment) | Organism |
---|---|
column chromatography, gel filtration | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
AKR1C1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADP+ | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000059 | - |
3,5-dichlorosalicylic acid | wild type enzyme, in 0.1 M potassium phosphate buffer, pH 7.4 | Homo sapiens | |
0.00027 | - |
3,5-dichlorosalicylic acid | mutant enzyme L306A, in 0.1 M potassium phosphate buffer, pH 7.4 | Homo sapiens | |
0.00058 | - |
3,5-dichlorosalicylic acid | mutant enzyme H222S, in 0.1 M potassium phosphate buffer, pH 7.4 | Homo sapiens | |
0.00085 | - |
3,5-dichlorosalicylic acid | mutant enzyme L54V, in 0.1 M potassium phosphate buffer, pH 7.4 | Homo sapiens | |
0.0028 | - |
3,5-dichlorosalicylic acid | mutant enzyme L308A, in 0.1 M potassium phosphate buffer, pH 7.4 | Homo sapiens |