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Literature summary extracted from

  • Contractor, T.; Harris, C.R.
    p53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2 (2012), Cancer Res., 72, 560-567.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.2 acetyl-CoA Pdk2-specific activity increases if acetyl-CoA and NADH levels increase, but decreases if pyruvate levels increase Homo sapiens
2.7.11.2 NADH Pdk2-specific activity increases if acetyl-CoA and NADH levels increase, but decreases if pyruvate levels increase Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.2 expression in HCT-116 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.2 P53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2 Homo sapiens
2.7.11.2 P53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2 Mus musculus
2.7.11.2 pyruvate Pdk2-specific activity increases if acetyl-CoA and NADH levels increase, but decreases if pyruvate levels increase Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.2 Mg2+ rquired Mus musculus
2.7.11.2 Mg2+ rquired 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 (acetyl-transferring)] Mus musculus
-
 ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate
-
 ?
2.7.11.2 ATP + [pyruvate dehydrogenase (acetyl-transferring)] Homo sapiens
-
 ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.2 Homo sapiens
-
-
-
2.7.11.2 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.2 carcinoma cell
-
 Mus musculus
-
2.7.11.2 carcinoma cell
-
 Homo sapiens
-
2.7.11.2 EB-1 cell
-
 Homo sapiens
-
2.7.11.2 HCT-116 cell
-
 Homo sapiens
-
2.7.11.2 MCF-7 cell MCF-7 cells do not express mRNA for pdk4, but express Pdk2 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.2 ATP + [pyruvate dehydrogenase (acetyl-transferring)]
-
 Mus musculus ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate
-
 ?
2.7.11.2 ATP + [pyruvate dehydrogenase (acetyl-transferring)]
-
 Homo sapiens ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDK2
-
 Mus musculus
2.7.11.2 PDK2
-
 Homo sapiens
2.7.11.2 pyruvate dehydrogenase kinase
-
 Mus musculus
2.7.11.2 pyruvate dehydrogenase kinase
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.2 ATP
-
 Mus musculus
2.7.11.2 ATP
-
 Homo sapiens

Expression

EC Number Organism Comment Expression
2.7.11.2 Homo sapiens Pdk2 transcription decreases upon addition of nutlin-3a, nutlin-3a can produce off-target effects, upon reduction of p53, the effect of nutlin-3a upon Pdk2 protein decreases. A histone deacetylase inhibitor, trichostatin A, partially prevents repression of Pdk2 transcription by p53 down
2.7.11.2 Mus musculus the amount of Pdk2 mRNA in both colon and spleen decreases upon irradiation of wild-type mice but not upon irradiation of p53 knockout mice, p53 decreases Pdk2 transcription in vivo down
2.7.11.2 Homo sapiens cotransfection with plasmids expressing either E2F1 or E2F2 activates Pdk2/luciferase transcription. E2F1 binds less well to the Pdk2 promoter when p53 is induced with zinc up

General Information

EC Number General Information Comment Organism
2.7.11.2 metabolism p53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2, which negatively regulates the pyruvate dehydrogenase complex. Decreased levels of Pdk2 and P-Pdc in turn promote conversion of pyruvate into acetyl-CoA instead of lactate Mus musculus
2.7.11.2 metabolism p53 negatively regulates transcription of the pyruvate dehydrogenase kinase Pdk2, which negatively regulates the pyruvate dehydrogenase complex. Decreased levels of Pdk2 and P-Pdc in turn promote conversion of pyruvate into acetyl-CoA instead of lactate Homo sapiens
2.7.11.2 physiological function Pdk2 is seen as the key control point in conversion of pyruvate to acetyl-CoA reaction because it responds allosterically to rapid local changes in substrate and product: Pdk2-specific activity increases if acetyl-CoA and NADH levels increase, but decreases if pyruvate levels increase Mus musculus
2.7.11.2 physiological function Pdk2 is seen as the key control point in conversion of pyruvate to acetyl-CoA reaction because it responds allosterically to rapid local changes in substrate and product: Pdk2-specific activity increases if acetyl-CoA and NADH levels increase, but decreases if pyruvate levels increase. P53-dependent apoptosis requires downregulation of Pdk2, early apoptotic events do not occur unless p53 can downregulate the transcription of Pdk2 Homo sapiens