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Literature summary for 2.7.11.2 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
Search for more literature for 2.7.11.2

Activating Compound

Activating Compound Comment Organism Structure
dihydrolipoyl transacetylase requirement Rattus norvegicus

Cloned(Commentary)

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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

Organism UniProt Comment Textmining
Rattus norvegicus
-
 isozymes PDK1 and PDK2
-

Purification (Commentary)

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + Ac-YHGHSMSDPGVSYR recombinant enzyme Rattus norvegicus ADP + [Ac-YHGHSMSDPGVSYR]phosphate
-
 ?
ATP + Ac-YHGHSMSDPGVSYR synthetic peptide substrate Rattus norvegicus ADP + [Ac-YHGHSMSDPGVSYR]phosphate
-
 ?
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
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
additional information performs autophosphorylation Rattus norvegicus ?
-
 ?

Synonyms

Synonyms Comment Organism
PDK
-
 Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP dependent on Rattus norvegicus