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Literature summary extracted from

  • Zheng, X.; Zhang, L.; Zhai, J.; Chen, Y.; Luo, H.; Hu, X.
    The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase (2012), FEBS Lett., 586, 55-59.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.21 expression of His6-tagged ALR2 in Escherichia coli Homo sapiens

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.21 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

EC Number Inhibitors Comment Organism Structure
1.1.1.21 epalrestat
-
 Homo sapiens
1.1.1.21 indomethacin
-
 Homo sapiens
1.1.1.21 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
1.1.1.21 sulindac sulfide enzyme binding structure, overview Homo sapiens
1.1.1.21 sulindac sulfone enzyme binding structure, overview Homo sapiens
1.1.1.21 Tolmetin enzyme binding structure, overview Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Homo sapiens P15121
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 DL-glyceraldehyde + NADPH substrate of aldose reductase ALR2 Homo sapiens glycerol + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldose reductase
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.1.1.21 6.2
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.1.1.21 0.0003
-
 sulindac sulfide pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens
1.1.1.21 0.000434
-
 sulindac sulfone pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens
1.1.1.21 0.000458
-
 sulindac pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.00011
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens epalrestat
1.1.1.21 0.000279
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens sulindac sulfide
1.1.1.21 0.000367
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens sulindac sulfone
1.1.1.21 0.000374
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens sulindac
1.1.1.21 0.00239
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens Tolmetin
1.1.1.21 0.00928
-
 pH 6.2, temperature not specified in the publication, ALR2 Homo sapiens indomethacin