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Literature summary for 1.2.1.104 extracted from

  • Nemeria, N.S.; Korotchkina, L.G.; Chakraborty, S.; Patel, M.S.; Jordan, F.
    Acetylphosphinate is the most potent mechanism-based substrate-like inhibitor of both the human and Escherichia coli pyruvate dehydrogenase components of the pyruvate dehydrogenase complex (2006), Bioorg. Chem., 34, 362-379.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.2.1.104

Protein Variants

Protein Variants Comment Organism
H63A about 17% residual activity in assay using 2,6-dichlorophenolindophenol, only modest inhibition by acetylphosphinate and acetylmethylphosphinate Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetylmethylphosphinate partially reversible tight-binding inhibitor, formation of a C2alpha-phosphinolactylthiamine diphosphate derivative involving H63 residue of enzyme Escherichia coli
acetylmethylphosphinate partially reversible tight-binding inhibitor, formation of a C2alpha-phosphinolactylthiamine diphosphate derivative involving H63 residue of enzyme Homo sapiens
Acetylphosphinate partially reversible tight-binding inhibitor, formation of a C2alpha-phosphinolactylthiamine diphosphate derivative involving H63 residue of enzyme Escherichia coli
Acetylphosphinate partially reversible tight-binding inhibitor, formation of a C2alpha-phosphinolactylthiamine diphosphate derivative involving H63 residue of enzyme Homo sapiens

Organism

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pyruvate + acetylphosphinate + NAD+
-
 Homo sapiens (R)-acetoin + ? + NADH
-
 ?
pyruvate + acetylphosphinate + NAD+
-
 Escherichia coli (S)-acetoin + ? + NADH
-
 ?
pyruvate + CoA + NAD+
-
 Escherichia coli acetyl-CoA + CO2 + NADH
-
 ?
pyruvate + CoA + NAD+
-
 Homo sapiens acetyl-CoA + CO2 + NADH
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000014
-
 Acetylphosphinate pH 8.0, 30°C Homo sapiens
0.00076
-
 Acetylphosphinate pH 8.0, 30°C Escherichia coli
0.00146
-
 acetylmethylphosphinate pH 8.0, 30°C Homo sapiens
0.0033
-
 acetylmethylphosphinate pH 8.0, 30°C Escherichia coli