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Literature summary for 1.2.1.104 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
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Protein Variants

Protein Variants Comment Organism
Y177A 11% residual pyruvate dehydrogenase multienzyme complex activity, binding of thiamine diphosphate is unaffected Escherichia coli
Y177F 7% residual pyruvate dehydrogenase multienzyme complex activity Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
thiamin 2-thiazolone diphosphate tight-binding inhibitor, binds via a two-step mechanism, Escherichia coli
thiamin 2-thiothiazolone diphosphate tight-binding inhibitor, binds via a two-step mechanism to wild-type, but to mutant Y177A via a one-step mechanism Escherichia coli

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00158
-
 thiamine diphosphate wild-type, Hill coefficient 1.38, pH 7.0, 30°C Escherichia coli
0.00665
-
 thiamine diphosphate mutant Y177A, Hill coefficient 1.0, pH 7.0, 30°C Escherichia coli
0.28
-
 pyruvate mutant Y177A, pH 7.0, 30°C Escherichia coli
0.515
-
 pyruvate wild-type, pH 7.0, 30°C Escherichia coli
0.531
-
 pyruvate mutant Y177F, pH 7.0, 30°C Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli P0AFG8 P0AFG8 i.e. pyruvate dehydrogenase E1 component, cf. EC 1.2.4.1
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pyruvate + CoA + dichlorophenol indophenol
-
 Escherichia coli acetyl-CoA + CO2 + ?
-
 ?
pyruvate + CoA + thiamine diphosphate
-
 Escherichia coli acetyl-CoA + CO2 + ?
-
 ?

Synonyms

Synonyms Comment Organism
aceE
-
 Escherichia coli

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.31
-
 thiamine diphosphate mutant Y177A, Hill coefficient 1.0, pH 7.0, 30°C Escherichia coli
28.89
-
 thiamine diphosphate wild-type, Hill coefficient 1.38, pH 7.0, 30°C Escherichia coli

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
12
-
 pyruvate mutant Y177A, pH 7.0, 30°C Escherichia coli
56
-
 pyruvate wild-type, pH 7.0, 30°C Escherichia coli
498
-
 thiamine diphosphate mutant Y177A, Hill coefficient 1.0, pH 7.0, 30°C Escherichia coli
18000
-
 thiamine diphosphate wild-type, Hill coefficient 1.38, pH 7.0, 30°C Escherichia coli