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Literature summary extracted from

  • Piao, L.; Sidhu, V.K.; Fang, Y.H.; Ryan, J.J.; Parikh, K.S.; Hong, Z.; Toth, P.T.; Morrow, E.; Kutty, S.; Lopaschuk, G.D.; Archer, S.L.
    FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4 (PDK4) decreases glucose oxidation and impairs right ventricular function in pulmonary hypertension: therapeutic benefits of dichloroacetate (2013), J. Mol. Med., 91, 333-346.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.2 Dichloroacetate the PDK inhibitor restores pyruvate dehydrogenae activity and enhances glucose oxidation with beneficial molecular effects, i.e. downregulation of FOXO-1 and PDK4, and functional improvement,i.e. enhanced right ventricular function and exercise capacity Homo sapiens
2.7.11.2 Dichloroacetate the PDK inhibitor restores pyruvate dehydrogenae activity and enhances glucose oxidation with beneficial molecular effects, i.e. downregulation of FOXO-1 and PDK4, and functional improvement,i.e. enhanced right ventricular function and exercise capacity Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.2 Homo sapiens
-
-
-
2.7.11.2 Rattus norvegicus
-
-
-
2.7.11.2 Rattus norvegicus Fawn-Hooded
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.2 heart
-
 Homo sapiens
-
2.7.11.2 heart
-
 Rattus norvegicus
-
2.7.11.2 lung
-
 Homo sapiens
-
2.7.11.2 lung
-
 Rattus norvegicus
-

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDK4
-
 Homo sapiens
2.7.11.2 PDK4
-
 Rattus norvegicus
2.7.11.2 pyruvate dehydrogenase kinase-4
-
 Homo sapiens
2.7.11.2 pyruvate dehydrogenase kinase-4
-
 Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.2 ATP
-
 Homo sapiens
2.7.11.2 ATP
-
 Rattus norvegicus

Expression

EC Number Organism Comment Expression
2.7.11.2 Homo sapiens FOXO1-mediated 4fold upregulation of pyruvate dehydrogenase kinase-4. Pyruvate dehydrogenase kinase is activated in right ventricular hypertrophy, causing an increase in glycolysis relative to glucose oxidation that impairs right ventricular function. Chronic dichloroacetate inhibits FOXO1-induced PDK4 upregulation and restores gluccoe oxidation up
2.7.11.2 Rattus norvegicus FOXO1-mediated 4fold upregulation of pyruvate dehydrogenase kinase-4. Pyruvate dehydrogenase kinase is activated in right ventricular hypertrophy, causing an increase in glycolysis relative to glucose oxidation that impairs right ventricular function. Chronic dichloroacetate inhibits FOXO1-induced PDK4 upregulation and restores gluccoe oxidation up

General Information

EC Number General Information Comment Organism
2.7.11.2 malfunction FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4 decreases glucose oxidation and impairs right ventricular function in pulmonary hypertension, overview. The bioenergetic impairment and right ventricular dysfunction can be reversed by dichloroacetate Homo sapiens
2.7.11.2 malfunction FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4 decreases glucose oxidation and impairs right ventricular function in pulmonary hypertension, overview. The bioenergetic impairment and right ventricular dysfunction can be reversed by dichloroacetate Rattus norvegicus
2.7.11.2 physiological function expression of PDK4 is regulated by its regulatory transcription factor, FOXO1. FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4. Pyruvate dehydrogenase kinase is activated in right ventricular hypertrophy, causing an increase in glycolysis relative to glucose oxidation that impairs right ventricular function. Chronic dichloroacetate inhibits FOXO1-induced PDK4 upregulation and restores gluccoe oxidation Homo sapiens
2.7.11.2 physiological function expression of PDK4 is regulated by its regulatory transcription factor, FOXO1. FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4. Pyruvate dehydrogenase kinase is activated in right ventricular hypertrophy, causing an increase in glycolysis relative to glucose oxidation that impairs right ventricular function. Chronic dichloroacetate inhibits FOXO1-induced PDK4 upregulation and restores gluccoe oxidation Rattus norvegicus