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 | 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 | 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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozymes PDHK1, PDHK2, PDHK3, and PDHK4 | - |
Rattus norvegicus | - |
Wistar rats, isozymes PDHK1, PDHK2, PDHK3, and PDHK4 | - |
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 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 | 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 | Comment | Organism |
---|---|---|
PDH kinase | - |
Homo sapiens |
PDH kinase | - |
Rattus norvegicus |
PDHK | - |
Homo sapiens |
PDHK | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
30 | - |
assay at | Rattus norvegicus |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens | |
ATP | - |
Rattus norvegicus |
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 |