Cloned (Comment) | Organism |
---|---|
expression of His6-tagged ALR2 in Escherichia coli | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
purified recombinant His-tagged ALR2 in complex with inhibitors sulindac, sulindac sulfide, sulindac sulfone, and tolmetin, hanging drop vapor diffusion method, 25 mg/ml enzyme with two equivalents of NADP+ and 7.5% PEG 6000 were equilibrated against a well containing 1 ml of 120 mM ammonium citrate, pH 5.0, 20% m/v PEG 6000, soaking of crystals in inhibitor saturated solution containing 25% m/v PEG 6000, 50 mM ammonium citrate, pH 5.0, and 5% v/v DMSO, X-ray diffraction structure determination and analysis | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
epalrestat | - |
Homo sapiens | |
indomethacin | - |
Homo sapiens | |
sulindac | exhibits both the highest inhibitory activity towards human aldose reductase among popular non-steroidal anti-inflammatory drugs and clear beneficial clinical effects on Type 2 diabetes, uncompetitive inhibition, enzyme binding structure, overview | Homo sapiens | |
sulindac sulfide | enzyme binding structure, overview | Homo sapiens | |
sulindac sulfone | enzyme binding structure, overview | Homo sapiens | |
Tolmetin | enzyme binding structure, overview | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P15121 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
DL-glyceraldehyde + NADPH | substrate of aldose reductase ALR2 | Homo sapiens | glycerol + NADP+ | - |
? |
Synonyms | Comment | Organism |
---|---|---|
aldose reductase | - |
Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
6.2 | - |
assay at | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NADPH | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0003 | - |
sulindac sulfide | pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | |
0.000434 | - |
sulindac sulfone | pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | |
0.000458 | - |
sulindac | pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00011 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | epalrestat | |
0.000279 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | sulindac sulfide | |
0.000367 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | sulindac sulfone | |
0.000374 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | sulindac | |
0.00239 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | Tolmetin | |
0.00928 | - |
pH 6.2, temperature not specified in the publication, ALR2 | Homo sapiens | indomethacin |