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Literature summary for 2.7.11.2 extracted from

  • Kwon, H.S.; Harris, R.A.
    Mechanisms responsible for regulation of pyruvate dehydrogenase kinase 4 gene expression (2004), Adv. Enzyme Regul., 44, 109-121.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
glucocorticoids regulate the basal expression level of PDK4, bind to a glucorticoid response element GRE located in the proximal promotor requiring binding of FOXO proteins, FOXO protein binding to the GRE can be inhibited by insulin, glucocorticoids act synergistically with retinoic acid Homo sapiens
additional information glucocorticoids and insulin regulate the basal expression level of PDK4, starvation and diabetes mellitus increase PDK4 expression in most tissues, no effects by dexamethasone Rattus norvegicus
additional information histone acetylation and transcription activation of gene PDK4 by retinoic acid and trichostatin A, retinoic acid acts synergistically with glucocorticoids, induction by dexamethasone can be inhibited by RU486 Homo sapiens
additional information no effects on PDK4 expression level by dexamethasone Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
PDK4 gene is located in q21.3 region of chromosome 7, DNA sequence analysis, genomic organization, DNA sequence determination of the partial proximal promotor Homo sapiens
the gene encoding PDK4 is located on chromosome 4, DNA sequence analysis, genomic organization, possible regulatory important elements are Sp1 and CBF sites Rattus norvegicus
the gene encoding PDK4 is located on chromosome 6, DNA sequence analysis, genomic organization, possible regulatory important elements are Sp1 and CBF sites Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
additional information insulin regulate the basal expression level of PDK4 by inhibiting the glucocorticoid-dependent stimulation of PDK4 expression via inactivation of FOXO proteins, FOXO proteins bind to the insulin response element which is required for the glucocorticoid response Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Mus musculus PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, complex regulation and the molecular mechanisms ?
-
?
additional information Rattus norvegicus PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, complex regulation and the molecular mechanisms ?
-
?
additional information Homo sapiens PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, detailed overview and modeling of the complex regulation and the molecular mechanisms ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
isozyme PDK4
-
Rattus norvegicus
-
isozymes PDK1, PDK2, PDK3, and PDK4
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
Homo sapiens
-
Hep-G2 cell
-
Homo sapiens
-
hepatoma cell
-
Homo sapiens
-
hepatoma cell PDK4 Rattus norvegicus
-
kidney PDK2 Rattus norvegicus
-
L-6 myoblast cell muscle cell Rattus norvegicus
-
liver
-
Homo sapiens
-
liver PDK2 Rattus norvegicus
-
additional information starvation and diabetes mellitus increase PDK4 expression in most tissues, PDK2 especially in liver and kidney Rattus norvegicus
-
Morris hepatoma 7800C1 cell
-
Rattus norvegicus
-
skeletal muscle
-
Homo sapiens
-
skeletal muscle
-
Rattus norvegicus
-
T-lymphocyte
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + pyruvate dehydrogenase PDH inactivation by phosphorylation at serine residues of the E1alpha component of the complex Rattus norvegicus ADP + phosphorylated pyruvate dehydrogenase
-
?
additional information PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, complex regulation and the molecular mechanisms Mus musculus ?
-
?
additional information PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, complex regulation and the molecular mechanisms Rattus norvegicus ?
-
?
additional information PDK4 is critically important in the starved state because it helps prevent hypoglycemia, the enzyme is part of the pyruvate dehydrogenase complex PDC, detailed overview and modeling of the complex regulation and the molecular mechanisms Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
PDK1
-
Rattus norvegicus
PDK2
-
Rattus norvegicus
PDK3
-
Rattus norvegicus
PDK4
-
Mus musculus
PDK4
-
Homo sapiens
PDK4
-
Rattus norvegicus
pyruvate dehydrogenase kinase 4
-
Mus musculus
pyruvate dehydrogenase kinase 4
-
Homo sapiens
pyruvate dehydrogenase kinase 4
-
Rattus norvegicus