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Literature summary for 2.7.11.2 extracted from

  • Baker, J.C.; Yan, X.; Peng, T.; Kasten, S.; Roche, T.E.
    Marked differences between two isoforms of human pyruvate dehydrogenase kinase (2000), J. Biol. Chem., 275, 15773-15781.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
acetyl-CoA domain-specific binding, isozymes PDK2 and PDK3 Homo sapiens
acetyl-CoA synergism with NADH Homo sapiens
dihydrolipoyl transacetylase stimulation rates in different buffers, stimulating domains for the isozyme PDK2 and PDK3 differ, overview Homo sapiens
dihydrolipoyl transacetylase lipoylation is required for binding, structural mutants stimulate less Homo sapiens
NADH domain-specific binding, isozymes PDK2 and PDK3 Homo sapiens
NADH synergism with acetyl-CoA Homo sapiens
phosphate isozyme PDK43, direct inhibition and elevation of the Km for ATP Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
isozymes PDK2 and PDK3, expression in Escherichia coli BL21(DE3) as His-tagged proteins Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
ADP 50-60% inhibition of isozyme PDK3, in presence of dihydrolipoyl transacetylase 70% Homo sapiens
Dichloroacetate inhibition of isozyme PDK3 is independent of dihydrolipoyl transacetylase, while isozyme PDK2 is more sensitive to inhibition when bound to it Homo sapiens
additional information carnitine, acetylcarnitine, malate, spermine, and calcium have no effect on isozyme PDK3 in presence of dihydrolipoyl transacetylase Homo sapiens
thiamine diphosphate
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.006
-
ATP isozyme PDK2, 30°C, pH 7.3, MOPS-K+ buffer Homo sapiens
0.006
-
ATP isozyme PDK3, 30°C, pH 7.3, Tris-HEPES buffer Homo sapiens
0.013
-
ATP isozyme PDK3, 30°C, pH 7.3, MOPS-K+ buffer Homo sapiens
0.023
-
ATP isozyme PDK2, 30°C, pH 7.3, Tris-HEPES buffer Homo sapiens
0.029
-
ATP isozyme PDK3, 30°C, pH 7.3, phosphate buffer Homo sapiens
0.04
-
ATP isozyme PDK2, 30°C, pH 7.3, phosphate buffer Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
45806
-
x * 45806, recombinant isozyme PDK2, detagged, amino acid determination Homo sapiens
46504
-
x * 46504, recombinant isozyme PDK3, detagged, amino acid determination Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + [pyruvate dehydrogenase (lipoamide)] Homo sapiens catalyzes inactivation through phosphorylation of pyruvate dehydrogenase complex EC 1.2.4.1 ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozymes PDK2 and PDK3
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged isozymes PDK2 and PDK3 from Escherichia coli BL21(DE3) Homo sapiens

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.44
-
isozyme PDK3, pH 7.3, 30°C Homo sapiens
0.69
-
isozyme PDK2, pH 7.3, 30°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [pyruvate dehydrogenase (lipoamide)]
-
Homo sapiens ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir
ATP + [pyruvate dehydrogenase (lipoamide)] catalyzes inactivation through phosphorylation of pyruvate dehydrogenase complex EC 1.2.4.1 Homo sapiens ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir

Subunits

Subunits Comment Organism
? x * 45806, recombinant isozyme PDK2, detagged, amino acid determination Homo sapiens
? x * 46504, recombinant isozyme PDK3, detagged, amino acid determination Homo sapiens

Synonyms

Synonyms Comment Organism
PDK
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at Homo sapiens
30
-
phosphate buffer Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7 7.4 assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP dependent on Homo sapiens