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Literature summary extracted from

  • Nemeria, N.; Yan, Y.; Zhang, Z.; Brown, A.M.; Arjunan, P.; Furey, W.; Guest, J.R.; Jordan, F.
    Inhibition of the Escherichia coli pyruvate dehydrogenase complex E1 subunit and its tyrosine 177 variants by thiamin 2-thiazolone and thiamin 2-thiothiazolone diphosphates. Evidence for reversible tight-binding inhibition (2001), J. Biol. Chem., 276, 45969-45978.
    View publication on PubMed

Protein Variants

EC Number Protein Variants Comment Organism
1.2.4.1 Y177A 11% of wild-type activity in enzyme complex Escherichia coli
1.2.4.1 Y177F 7% of wild-type activity in enzyme complex Escherichia coli

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.2.4.1 thiamine 2-thiothiazolone diphosphate
-
 Escherichia coli
1.2.4.1 thiamine 2-thiothiazolone diphosphate
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.2.4.1 0.00158
-
 thiamine diphosphate wild-type enzyme Escherichia coli
1.2.4.1 0.00665
-
 thiamine diphosphate Y177A mutant enzyme Escherichia coli
1.2.4.1 0.28
-
 pyruvate Y177A mutant enzyme Escherichia coli
1.2.4.1 0.515
-
 pyruvate wild-type enzyme Escherichia coli
1.2.4.1 0.531
-
 pyruvate Y177F mutant enzyme Escherichia coli

Organism

EC Number Organism UniProt Comment Textmining
1.2.4.1 Escherichia coli
-
-
-
1.2.4.1 Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
1.2.4.1 0.0048
-
 Y177A mutant enzyme, 2,6-dichlorophenolindophenol assay, substrate 2alpha-hydroxyethyl-thiamin diphosphate Escherichia coli
1.2.4.1 0.00671
-
 Y177F mutant enzyme, 2,6-dichlorophenolindophenol assay, substrate 2alpha-hydroxyethyl-thiamin diphosphate Escherichia coli
1.2.4.1 0.0098
-
 wild-type enzyme, 2,6-dichlorophenolindophenol assay, substrate 2alpha-hydroxyethyl-thiamin diphosphate Escherichia coli
1.2.4.1 0.087
-
 Y177A mutant enzyme, 2,6-dichlorophenolindophenol assay, substrate pyruvate Escherichia coli
1.2.4.1 0.216
-
 Y177F mutant enzyme, 2,6-dichlorophenolindophenol assay, substrate pyruvate Escherichia coli
1.2.4.1 0.445
-
 wild-type enzyme, 2,6-dichlorophenolindophenol assay, substrate pyruvate Escherichia coli

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.2.4.1 acetaldehyde + benzaldehyde
-
 Escherichia coli (R)-phenylacetylcarbinol
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.2.4.1 0.000003
-
 thiamine 2-thiazolone diphosphate
-
 Escherichia coli
1.2.4.1 0.000064
-
 thiamine 2-thiothiazolone diphosphate
-
 Escherichia coli
1.2.4.1 0.0000737
-
 thiamine 2-thiothiazolone diphosphate
-
 Homo sapiens