Literature summary for 1.2.4.1 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.

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Protein Variants

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

Inhibitors

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

KM Value [mM]

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

Organism

Organism	UniProt	Comment	Textmining
Escherichia coli	-	-	-
Homo sapiens	-	-	-

Specific Activity [micromol/min/mg]

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

Substrates and Products (Substrate)

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

Ki Value [mM]

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

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Release 2023.1 (January 2023)