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Literature summary for 1.1.1.21 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)

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

Crystallization (Commentary)

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

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

Organism UniProt Comment Textmining
Homo sapiens P15121
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
aldose reductase
-
Homo sapiens

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

Ki Value [mM]

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 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