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Literature summary for 2.7.11.2 extracted from
- R-lipoic acid inhibits mammalian pyruvate dehydrogenase kinase (2004), Free Radic. Res., 38, 1083-1092.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| additional information | the enzyme is stimulated by reduction or reduction/acetylation of the lipoyl moieties of pyruvate dehydrogenase complex component E2 | Homo sapiens | |
| additional information | the enzyme is stimulated by reduction or reduction/acetylation of the lipoyl moieties of pyruvate dehydrogenase complex component E2 | Rattus norvegicus |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| His-tagged PDK3 overexpression in Escherichia coli strain BL21 | Homo sapiens |
| individual overexpressions of His-tagged isozymes PDK1, PDK2, and PDK4 in Escherichia coli strain BL21 | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| ADP | product inhibition, synergistic with pyruvate | Homo sapiens |  |
| ADP | product inhibition, synergistic with pyruvate | Rattus norvegicus | |
| dihydrolipoic acid | inhibits the activity of PDK3 towards the reconstituted PD complex slightly, but the activity towards E1 alone completely, inhibition mechanism | Homo sapiens | |
| dihydrolipoic acid | inhibits the activity of PDK1 towards the reconstituted PD complex, inhibition mechanism | Rattus norvegicus | |
| additional information | pyruvamide is a poor inhibitor of PDK3 | Homo sapiens | |
| Pyruvamide | inhibition of isozymes PDK1, PDK2, and PDK4 | Rattus norvegicus | |
| pyruvate | slight product inhibition, synergistic with ADP | Homo sapiens | |
| pyruvate | product inhibition, synergistic with ADP | Rattus norvegicus | |
| R-lipoic acid | inhibits isozyme PDK3 activity in the reconstituted PD complex, but not towards E1 alone, inhibition mechanism | Homo sapiens | |
| R-lipoic acid | inhibits isozymes PDK1, PDK2, and PDK4 activities in the reconstituted PD complex and towards E1 alone, inhibition mechanism, overview | Rattus norvegicus | |
| S-lipoic acid | inhibits isozyme PDK3 activity in the reconstituted PD complex, but not towards E1 alone, inhibition mechanism | Homo sapiens | |
| S-lipoic acid | inhibits isozymes PDK1, PDK2, and PDK4 activities in the reconstituted PD complex and towards E1 alone, inhibition mechanism, overview | Rattus norvegicus | |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Mg2+ | - |
Homo sapiens | |
| Mg2+ | - |
Rattus norvegicus | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + pyruvate dehydrogenase | Homo sapiens | - |
ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | Rattus norvegicus | - |
ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
isozyme PDK3 | - |
| Rattus norvegicus | - |
isozymes PDK1, PDK2, and PDK4 | - |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| phosphoprotein | PDK2 performs autophosphorylation in presence of R-lipoic acid | Rattus norvegicus |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged isozymes PDK1, PDK2, and PDK4 from Escherichia coli strain BL21 | Rattus norvegicus |
| recombinant His-tagged PDK3 from Escherichia coli strain BL21 | Homo sapiens |
Renatured (Commentary)
| Renatured (Comment) | Organism |
|---|---|
| reconstitution of the active pyruvate dehydrogenase complex PDC | Homo sapiens |
| reconstitution of the active pyruvate dehydrogenase complex PDC | Rattus norvegicus |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.006 | - |
PDK3 activity with E1 | Homo sapiens |
| 0.027 | - |
PDK2 activity with E1 | Rattus norvegicus |
| 0.031 | - |
PDK1 activity with E1 | Rattus norvegicus |
| 0.032 | - |
PDK4 activity with E1 | Rattus norvegicus |
| 0.038 | - |
PDK4 activity with reconstituted PDC | Rattus norvegicus |
| 0.056 | - |
PDK1 activity with reconstituted PDC | Rattus norvegicus |
| 0.064 | - |
PDK3 activity with reconstituted PDC | Homo sapiens |
| 0.087 | - |
PDK2 activity with reconstituted PDC | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + pyruvate dehydrogenase | - |
Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | - |
Rattus norvegicus | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | PDK activity as component of the pyruvate dehydrogenase complex PDC binding the lipoyl domain of E2 | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | PDK activity as component of the pyruvate dehydrogenase complex PDC binding the lipoyl domain of E2 | Rattus norvegicus | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | PDK is a component of the pyruvate dehydrogenase complex PDC binding the lipoyl domain of E2 | Homo sapiens |
| More | PDK is a component of the pyruvate dehydrogenase complex PDC binding the lipoyl domain of E2 | Rattus norvegicus |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDK1 | - |
Rattus norvegicus |
| PDK2 | - |
Rattus norvegicus |
| PDK3 | - |
Homo sapiens |
| PDK4 | - |
Rattus norvegicus |
| pyruvate dehydrogenase kinase | - |
Homo sapiens |
| pyruvate dehydrogenase kinase | - |
Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
| 30 | - |
assay at | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7 | - |
assay at | Homo sapiens |
| 7 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| ATP | - |
Rattus norvegicus | |
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Release 2023.1 (January 2023)
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