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Literature summary extracted from

  • Abbot, E.L.; McCormack, J.G.; Reynet, C.; Hassall, D.G.; Buchan, K.W.; Yeaman, S.J.
    Diverging regulation of pyruvate dehydrogenase kinase isoform gene expression in cultured human muscle cells (2005), FEBS J., 272, 3004-3014.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.2 additional information agonist activation of peroxisome proliferator-activated receptors alpha and delta specifically upregulates PDK4 transcription, while activation of peroxisome proliferator-activated receptor gamma specifically downregulates PDK2 transcription, reduced glucose levels increase expression levels of PDK2 and PDK4, the stimulation effect is reversed by insulin, insulin alone decreases the enzyme expression levels below basal values Homo sapiens
2.7.11.2 oleate activates PDK2 and PDK4 nearly 2fold at 0.1 mM, not synergistic with palmitate, stimulation is completely inhibited by insulin at 0.001 mM Homo sapiens
2.7.11.2 palmitate activates PDK2 and PDK4 nearly 2fold at 0.1 mM, not synergistic with oleate, stimulation is completely inhibited by insulin at 0.001 mmM Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.2 expression analysis and mRNA level determination for isozymes PDK2 and PDK4 in response to several effectors Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.2 additional information insulin reverses the stimulation effect of reduced glucose levels increasing expression levels of PDK2 and PDK4, insulin alone decreases the enzyme expression levels below basal values, insulin effects on the enzyme are inhibited by phosphoatidyl 3-kinase inhibitors wortmannin and LY294002, i.e. 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one Homo sapiens
2.7.11.2 Rapamycin inhibits PDK2 and PDK4, has no effect on insulin-caused downregulation of the isozymes 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 additional information Homo sapiens peroxisome proliferator-activated receptors and insulin have regulatory functions in expression of isozymes PDK2 and PDK4, regulation mechanism ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.2 Homo sapiens
-
 isozymes PDK1-4
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.2 cell culture
-
 Homo sapiens
-
2.7.11.2 muscle cell
-
 Homo sapiens
-
2.7.11.2 myoblast
-
 Homo sapiens
-
2.7.11.2 myotube
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.2 additional information peroxisome proliferator-activated receptors and insulin have regulatory functions in expression of isozymes PDK2 and PDK4, regulation mechanism Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDK1
-
 Homo sapiens
2.7.11.2 PDK2
-
 Homo sapiens
2.7.11.2 PDK3
-
 Homo sapiens
2.7.11.2 PDK4
-
 Homo sapiens
2.7.11.2 pyruvate dehydrogenase kinase
-
 Homo sapiens