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Literature summary extracted from

  • Mann, W.R.; Dragland, C.J.; Vinluan, C.C.; Vedananda, T.R.; Bell, P.A.; Aicher, T.D.
    Diverse mechanisms of inhibition of pyruvate dehydrogenase kinase by structurally distinct inhibitors (2000), Biochim. Biophys. Acta, 1480, 283-292.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.7.11.2 dihydrolipoyl transacetylase requirement Rattus norvegicus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.2 expression of His-tagged isozymes PDK1 and PDK2 in Escherichia coli BL21(DE3) Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.2 (R)-3,3,3-trifluoro-2-hydroxy-2-methylpropioamide strong inhibition, isozymes PDK1 and PDK2, inhibition mechanism Rattus norvegicus
2.7.11.2 adenosine 5'-[beta,gamma,imido]triphosphate isozymes PDK1 and PDK2, inhibition mechanism Rattus norvegicus
2.7.11.2 Dichloroacetate
-
Rattus norvegicus
2.7.11.2 dichloroacetophenone isozymes PDK1 and PDK2, inhibition mechanism Rattus norvegicus
2.7.11.2 lactone derivative of dichloroacetophenone isozymes PDK1 and PDK2, inhibition mechanism Rattus norvegicus
2.7.11.2 triterpenes isozymes PDK1 and PDK2, inhibition mechanism Rattus norvegicus

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 (lipoamide)] Rattus norvegicus catalyzes inactivation through phosphorylation of pyruvate dehydrogenase complex EC 1.2.4.1 ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.2 Rattus norvegicus
-
isozymes PDK1 and PDK2
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.2 recombinant His-tagged isozymes PDK1 and PDK2 expressed in Escherichia coli BL21(DE3) Rattus norvegicus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.2 ATP + Ac-YHGHSMSDPGVSYR recombinant enzyme Rattus norvegicus ADP + [Ac-YHGHSMSDPGVSYR]phosphate
-
?
2.7.11.2 ATP + Ac-YHGHSMSDPGVSYR synthetic peptide substrate Rattus norvegicus ADP + [Ac-YHGHSMSDPGVSYR]phosphate
-
?
2.7.11.2 ATP + [pyruvate dehydrogenase (lipoamide)] pyruvate dehydrogenase complex substrate is inactivated by ATP-dependent phosphorylation of 3 serine residues on the E1 subunit Rattus norvegicus ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir
2.7.11.2 ATP + [pyruvate dehydrogenase (lipoamide)] catalyzes inactivation through phosphorylation of pyruvate dehydrogenase complex EC 1.2.4.1 Rattus norvegicus ADP + [pyruvate dehydrogenase (lipoamide)] phosphate
-
ir
2.7.11.2 additional information performs autophosphorylation Rattus norvegicus ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDK
-
Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.2 ATP dependent on Rattus norvegicus