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Literature summary for 1.1.1.10 extracted from

  • El-Kabbani, O.; Carbone, V.; Darmanin, C.; Ishikura, S.; Hara, A.
    Structure of the tetrameric form of human L-xylulose reductase: probing the inhibitor-binding site with molecular modeling and site-directed mutagenesis (2005), Proteins, 60, 424-432.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
structure of the biological tetramer of human L-xylulose reductase in complex with NADP+ and the competitive inhibitor 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide, vapor diffusion method Homo sapiens

Protein Variants

Protein Variants Comment Organism
H146L IC50-value for 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide is 7.8fold higher than wild-type value, IC50-value for 4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide is 6.7fold higher than wild-type value Rattus norvegicus
L143F IC50-value for 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide is 8.3fold higher than wild-type value, IC50-value for 4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide is 1.9fold higher than wild-type value Rattus norvegicus
W191F IC50-value for 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide is 3.4fold higher than wild-type value, IC50-value for 4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide is 7.3fold higher than wild-type value Rattus norvegicus
W191S IC50-value for 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide is 13fold higher than wild-type value, IC50-value for 4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide is 1.5fold lower than wild-type value Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide
-
Homo sapiens
4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide IC50: 0.00023 mM for wild-type enzyme, 0.0019 mM for mutant enzyme L143F, 0.0018 mM for mutant enzyme H146L, 0.0029 mM for mutant enzyme W191S, 0.00079 mM for mutant enzyme W191F Rattus norvegicus
4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide IC50: 0.0003 mM for wild-type enzyme, 0.00056 mM for mutant enzyme L143F, 0.002 mM for mutant enzyme H146L, 0.0002 mM for mutant enzyme W191S, 0.0022 mM for mutant enzyme W191F Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
xylitol + NADP+
-
Homo sapiens L-xylulose + NADPH + H+
-
r
xylitol + NADP+
-
Rattus norvegicus L-xylulose + NADPH + H+
-
r

Subunits

Subunits Comment Organism
tetramer
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens
NADP+
-
Rattus norvegicus
NADPH
-
Homo sapiens
NADPH
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00037
-
4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide competitive with respect to xylitol Homo sapiens
0.00044
-
4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide uncompetitive with respect to NADPH Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00023
-
IC50: 0.00023 mM for wild-type enzyme, 0.0019 mM for mutant enzyme L143F, 0.0018 mM for mutant enzyme H146L, 0.0029 mM for mutant enzyme W191S, 0.00079 mM for mutant enzyme W191F Rattus norvegicus 4-methyl-[1,2,3]-thiadiazole-5-carboxylic acid benzyloxyamide
0.0003
-
IC50: 0.0003 mM for wild-type enzyme, 0.00056 mM for mutant enzyme L143F, 0.002 mM for mutant enzyme H146L, 0.0002 mM for mutant enzyme W191S, 0.0022 mM for mutant enzyme W191F Rattus norvegicus 4-methylthiophene-2-carboxylic acid N'-(2,3,3-trichloroacryloyl)-hydrazide