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Literature summary for 2.7.11.2 extracted from
- PDH kinase inhibitors: a novel therapy for Type II diabetes? (2005), Biochem. Soc. Trans., 33, 367-370.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | increased glucose oxidation by inhibition of PDHK activity may be effective for increasing glucose utilization in diabetes treatment | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| AZD7545 | noncompetitive to ATP | Homo sapiens |  |
| AZD7545 | noncompetitive to ATP, IC50 values for isozymes PDHK1, PDHK2, and PDHK4 | Rattus norvegicus | |
| compound K | noncompetitive to ATP, IC50 values for isozymes PDHK1, PDHK2, and PDHK4 | Rattus norvegicus | |
| Dichloroacetate | noncompetitive to ATP | Rattus norvegicus | |
| additional information | isozyme-specific inhibition by AZD7545 analogues | Rattus norvegicus |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + pyruvate dehydrogenase | Homo sapiens | PDHK plays a key role in controlling the balance between glucose and lipid oxidation according to substrate supply, PDHK inhibition leads to increased PDH activity increasing glucose oxidation | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | Rattus norvegicus | PDHK plays a key role in controlling the balance between glucose and lipid oxidation according to substrate supply, PDHK inhibition leads to increased PDH activity increasing glucose oxidation | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
isozymes PDHK1, PDHK2, PDHK3, and PDHK4 | - |
| Rattus norvegicus | - |
Wistar rats, isozymes PDHK1, PDHK2, PDHK3, and PDHK4 | - |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| heart | - |
Rattus norvegicus | - |
| kidney | - |
Rattus norvegicus | - |
| liver | - |
Rattus norvegicus | - |
| additional information | tissue-specific isozyme distribution | Homo sapiens | - |
| additional information | tissue-specific isozyme distribution | Rattus norvegicus | - |
| pancreatic beta cell | - |
Homo sapiens | - |
| pancreatic beta cell | - |
Rattus norvegicus | - |
| skeletal muscle | - |
Homo sapiens | - |
| skeletal muscle | - |
Rattus norvegicus | - |
| tibialis anterior | - |
Rattus norvegicus | - |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| additional information | - |
PDH activity in zucker diabetic fatty rats, i.e. ZDF rats, as indicator for the degree of PDHK inhibition | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| ATP + pyruvate dehydrogenase | PDHK plays a key role in controlling the balance between glucose and lipid oxidation according to substrate supply, PDHK inhibition leads to increased PDH activity increasing glucose oxidation | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | PDHK plays a key role in controlling the balance between glucose and lipid oxidation according to substrate supply, PDHK inhibition leads to increased PDH activity increasing glucose oxidation | Rattus norvegicus | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | phosphorylation of 3 serine residues of the E2 domain, isozyme-specific activity | Homo sapiens | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
| ATP + pyruvate dehydrogenase | phosphorylation of 3 serine residues of the E2 domain, isozyme-specific activity | Rattus norvegicus | ADP + phosphorylated pyruvate dehydrogenase | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| PDH kinase | - |
Homo sapiens |
| PDH kinase | - |
Rattus norvegicus |
| PDHK | - |
Homo sapiens |
| PDHK | - |
Rattus norvegicus |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 30 | - |
assay at | Rattus norvegicus |
Cofactor
| Cofactor | Comment | Organism | Structure |
|---|---|---|---|
| ATP | - |
Homo sapiens | |
| ATP | - |
Rattus norvegicus | |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.2 | - |
Dichloroacetate | isozyme PDHK2, 30°C | Rattus norvegicus | |
| 0.5 | - |
Dichloroacetate | isozyme PDHK4, 30°C | Rattus norvegicus | |
| 1 | - |
Dichloroacetate | isozyme PDHK1, 30°C | Rattus norvegicus | |
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