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Literature summary for 2.7.11.2 extracted from
- Pyruvate dehydrogenase kinase isoform 2 activity limited and further inhibited by slowing down the rate of dissociation of ADP (2004), Biochemistry, 43, 13432-13441.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| L2 domain | inner lipoyl domain of the E2 component of PDC, activates PDK2 | Homo sapiens | |
| additional information | the enzyme is stimulated 3.45fold by NADH/NAD+ and/or acetyl-Co via reduction and reductive acetylation of the lipoyl moieties of pyruvate dehydrogenase complex component E2 dihydrolipoyl acetyltransferase requiring elevated levels of Cl- and K+, activation increases the kcat and Km for ATP | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| co-expression of PDK2, E2, and E3 as His-tagged proteins | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| adenosine 5'-[beta,gamma-imido]triphosphate | - |
Homo sapiens |  |
| ADP | product inhibition, competitive to ATP, synergistic with pyruvate, PDK2, ADP, and pyruvate form a dead-end complex | Homo sapiens | |
| pyruvate | product inhibition, synergistic with ADP, PDK2, ADP, and pyruvate form a dead-end complex | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Homo sapiens | |
| 0.0077 | - |
ATP | pH 7.4, 30°C, with oxidized E2 | Homo sapiens | |
| 0.0109 | - |
ATP | pH 7.4, 30°C, with oxidized E2, in presence of NADH/NAD+ | Homo sapiens | |
| 0.0113 | - |
ATP | pH 7.4, 30°C, with oxidized E2, in presence of 2 mM DTT | Homo sapiens | |
| 0.025 | 0.22 | ATP | pH 7.4, 30°C, PDK2, with substrate E2-bound E1, dependent on the assay conditions concerning buffer composition, overview | Homo sapiens | |
| 0.039 | - |
ATP | pH 7.4, 30°C, with reduced E2 | Homo sapiens | |
| 0.047 | - |
ATP | pH 7.4, 30°C, with reduced E2, in presence of NADH/NAD+ | Homo sapiens | |
| 1.16 | - |
ATP | pH 7.4, 30°C, with reduced E2, in presence of NADH/NAD+ and acetyl-CoA | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| mitochondrion | - |
Homo sapiens | 5739 | - |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Cl- | activates | Homo sapiens | |
| Cl- | required for stimulation of PDK2 by reduction and reductive acetylation of E2 | Homo sapiens | |
| K+ | activates | Homo sapiens | |
| K+ | required for stimulation of PDK2 by reduction and reductive acetylation of E2 | Homo sapiens | |
| Mg2+ | - |
Homo sapiens | |
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 | Homo sapiens | phosphorylation of E2-bound E1 | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| recombinant His-tagged PDK2, E2, and E3 by nickel affinity chromatography, the His-tag is removable | Homo sapiens |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| ATP + [pyruvate dehydrogenase (acetyl-transferring)] = ADP + [pyruvate dehydrogenase (acetyl-transferring)]phosphate | ordered reaction mechanism with ATP binding before E1 | Homo sapiens | |
| ATP + [pyruvate dehydrogenase (acetyl-transferring)] = ADP + [pyruvate dehydrogenase (acetyl-transferring)]phosphate | ordered reaction mechanism with ATP binding first, overview | Homo sapiens |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
- |
Homo sapiens |
| 0.02 | - |
about, with E2 bound to E1, 0.2 mM ATP | Homo sapiens |
| 0.03 | - |
about, with E2 bound to E1 in presence of NADH/NAD+ and acetyl-CoA, 0.2 mM ATP | Homo sapiens |
| 0.037 | - |
about, with free E2, 0.2 mM ATP | Homo sapiens |
| 0.066 | - |
about, with free E2 in presence of NADH/NAD+ and acetyl-CoA, 0.2 mM ATP | Homo sapiens |
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 | phosphorylation of E2-bound E1 | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | phosphorylation of E2-bound E1, higher activity with reduced E2, enzyme stimulation reduces the amount of bound ADP | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | the pyruvate dehydrogenase is a component of the pyruvate dehydrogenase complex, PDC | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| More | PDK is a component of the pyruvate dehydrogenase complex | Homo sapiens |
| More | PDK is a component of the pyruvate dehydrogenase complex PDC binding the lipoyl domain of E2 | Homo sapiens |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDK2 | - |
Homo sapiens |
| pyruvate dehydrogenase kinase | - |
Homo sapiens |
| pyruvate dehydrogenase kinase 2 | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.12 | - |
ATP | pH 7.4, 30°C, with oxidized E2 | Homo sapiens | |
| 0.17 | - |
ATP | pH 7.4, 30°C, with oxidized E2, in presence of 2 mM DTT | Homo sapiens | |
| 0.21 | - |
ATP | pH 7.4, 30°C, with oxidized E2, in presence of NADH/NAD+ | Homo sapiens | |
| 0.9 | 4.7 | ATP | pH 7.4, 30°C, PDK2, with substrate E2-bound E1, dependent on the assay conditions concerning buffer composition, overview | Homo sapiens | |
| 0.91 | - |
ATP | pH 7.4, 30°C, with reduced E2 | Homo sapiens | |
| 1.3 | - |
ATP | pH 7.4, 30°C, with reduced E2, in presence of NADH/NAD+ | Homo sapiens | |
| 3.15 | - |
ATP | pH 7.4, 30°C, with reduced E2, in presence of NADH/NAD+ and acetyl-CoA | Homo sapiens | |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Homo sapiens |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| ATP | ordered reaction mechanism with ATP | Homo sapiens | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
| 0.0031 | - |
adenosine 5'-[beta,gamma-imido]triphosphate | pH 7.4, 30°C, versus ATP | Homo sapiens | |
| 0.14 | 0.52 | ADP | pH 7.4, 30°C, versus ATP, dependent on the assay conditions concerning buffer composition, overview | Homo sapiens | |
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