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Literature summary 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

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

Cloned(Commentary)

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

Inhibitors

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

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.2 0.006
-
 ATP isozyme PDK2, 30°C, pH 7.3, MOPS-K+ buffer Homo sapiens
2.7.11.2 0.006
-
 ATP isozyme PDK3, 30°C, pH 7.3, Tris-HEPES buffer Homo sapiens
2.7.11.2 0.013
-
 ATP isozyme PDK3, 30°C, pH 7.3, MOPS-K+ buffer Homo sapiens
2.7.11.2 0.023
-
 ATP isozyme PDK2, 30°C, pH 7.3, Tris-HEPES buffer Homo sapiens
2.7.11.2 0.029
-
 ATP isozyme PDK3, 30°C, pH 7.3, phosphate buffer Homo sapiens
2.7.11.2 0.04
-
 ATP isozyme PDK2, 30°C, pH 7.3, phosphate buffer Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.2 Mg2+
-
 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
2.7.11.2 45806
-
 x * 45806, recombinant isozyme PDK2, detagged, amino acid determination Homo sapiens
2.7.11.2 46504
-
 x * 46504, recombinant isozyme PDK3, detagged, amino acid determination Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.2 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

EC Number Organism UniProt Comment Textmining
2.7.11.2 Homo sapiens
-
 isozymes PDK2 and PDK3
-

Purification (Commentary)

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

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.7.11.2 0.44
-
 isozyme PDK3, pH 7.3, 30°C Homo sapiens
2.7.11.2 0.69
-
 isozyme PDK2, pH 7.3, 30°C Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.2 ATP + [pyruvate dehydrogenase (lipoamide)]
-
 Homo sapiens ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
 ir
2.7.11.2 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

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

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDK
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.2 30
-
 assay at Homo sapiens
2.7.11.2 30
-
 phosphate buffer Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.2 7 7.4 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.2 ATP dependent on Homo sapiens