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Literature summary for 2.7.11.2 extracted from

  • Tso, S.C.; Kato, M.; Chuang, J.L.; Chuang, D.T.
    Structural determinants for cross-talk between pyruvate dehydrogenase kinase 3 and lipoyl domain 2 of the human pyruvate dehydrogenase complex (2006), J. Biol. Chem., 281, 27197-27204.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
lipoyl domain L2 L2 of the PDK3-containing pyruvate dehydrogenase complex induces a cross-tail conformation in PDK3, resulting in an opening of the active site cleft and the stimulation of kinase activity Homo sapiens

Protein Variants

Protein Variants Comment Organism
D164A site-directed mutagenesis of isozyme PDK3, the L2 binding is slightly reduced compared to the wild-type isozyme PDK3 Homo sapiens
D172A site-directed mutagenesis of isozyme PDK3, the L2 binding is slightly reduced compared to the wild-type isozyme PDK3 Homo sapiens
E162A site-directed mutagenesis of isozyme PDK3, the L2 binding is slightly reduced compared to the wild-type isozyme PDK3 Homo sapiens
E170A site-directed mutagenesis of isozyme PDK3, the L2 binding is reduced compared to the wild-type isozyme PDK3 Homo sapiens
E179A site-directed mutagenesis of isozyme PDK3, the L2 binding is reduced compared to the wild-type isozyme PDK3 Homo sapiens
F32A site-directed mutagenesis of isozyme PDK3 lipoyl-binding pocket, the mutant has lost its L2 binding and L2-stimulated PDK3 activity Homo sapiens
F35A site-directed mutagenesis of isozyme PDK3 lipoyl-binding pocket, the mutant has lost its L2 binding and L2-stimulated PDK3 activity Homo sapiens
F48A site-directed mutagenesis of isozyme PDK3 lipoyl-binding pocket, the mutant has lost its L2 binding and L2-stimulated PDK3 activity Homo sapiens
L140A site-directed mutagenesis of isozyme PDK3, the L2 binding is reduced compared to the wild-type isozyme PDK3 Homo sapiens
L27A site-directed mutagenesis of isozyme PDK3 lipoyl-binding pocket, the mutant has lost its L2 binding and L2-stimulated PDK3 activity Homo sapiens
additional information serial truncations of the isozyme PDK3 C-terminal tail region either impede or abolish the binding of wild-type L2 to the PDK3 mutants, resulting in the reduction or absence of L2-enhanced kinase activity, overview Homo sapiens
P142A site-directed mutagenesis of isozyme PDK3, the L2 binding is unaltered compared to the wild-type isozyme PDK3 Homo sapiens
R196A site-directed mutagenesis of isozyme PDK3, the L2 binding is slightly reduced compared to the wild-type isozyme PDK3 Homo sapiens
T175A site-directed mutagenesis of isozyme PDK3, the L2 binding is unaltered compared to the wild-type isozyme PDK3 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information kinetics and thermodynamics of PDK binding to L2 within the pyruvate dehydrogenase complex Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Homo sapiens 5739
-

Metals/Ions

Metals/Ions Comment Organism Structure
K+
-
Homo sapiens
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens pyruvate dehydrogenase kinase isozymes are the molecular switch that down-regulates activity of the pyruvate dehydrogenase complex through reversible phosphorylation ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
isozymes PDK1-4
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information pyruvate dehydrogenase kinase isozymes are the molecular switch that down-regulates activity of the pyruvate dehydrogenase complex through reversible phosphorylation Homo sapiens ?
-
?
additional information interaction of PDK with L2 within the pyruvate dehydrogenase complex, overview Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
More structural determinants for cross-talk between PDK3 and lipoyl domain 2 of the pyruvate dehydrogenase complex, overview Homo sapiens

Synonyms

Synonyms Comment Organism
PDK
-
Homo sapiens
pyruvate dehydrogenase kinase
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperature Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.3
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens