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Literature summary extracted from

  • Carbone, V.; Zhao, H.T.; Chung, R.; Endo, S.; Hara, A.; El-Kabbani, O.
    Correlation of binding constants and molecular modelling of inhibitors in the active sites of aldose reductase and aldehyde reductase (2009), Bioorg. Med. Chem., 17, 1244-1250.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.1.1.21 expressed in Escherichia coli cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 3,5-dichlorosalicylic acid uncompetitive inhibition Homo sapiens
1.1.1.21 minalrestat uncompetitive inhibition Homo sapiens
1.1.1.21 additional information Arg312 in ALR1 contributes favourably to the binding of 3,5-dichlorosalicylic acid through an electrostatic interaction with the inhibitor's electronegative halide atom and undergoes a conformational change upon tolrestat binding. Tyr116 in ALR1 forms electrostatic interactions with the fluorobenzyl moiety of minalrestat and the 3- and 4-hydroxy groups on the phenyl ring of quercetin. Homo sapiens
1.1.1.21 quercetin uncompetitive inhibition Homo sapiens
1.1.1.21 Tolrestat uncompetitive inhibition Homo sapiens

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
1.1.1.21 Blue Sepharose column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 DL-glyceraldehyde + NADPH + H+
-
 Homo sapiens glycerol + NADP+
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldose reductase
-
 Homo sapiens
1.1.1.21 ALR2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.00026
-
 ALR2 in 50 mM potassium phosphate (pH 6.2) Homo sapiens Tolrestat
1.1.1.21 0.00028
-
 ALR2 in 50 mM potassium phosphate (pH 6.2) Homo sapiens minalrestat
1.1.1.21 0.00592
-
 ALR2 in 50 mM potassium phosphate (pH 6.2) Homo sapiens quercetin
1.1.1.21 0.127
-
 ALR2 in 50 mM potassium phosphate (pH 6.2) Homo sapiens 3,5-dichlorosalicylic acid