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Literature summary extracted from

  • Mayers, R.M.; Leighton, B.; Kilgour, E.
    PDH kinase inhibitors: a novel therapy for Type II diabetes? (2005), Biochem. Soc. Trans., 33, 367-370.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.11.2 medicine increased glucose oxidation by inhibition of PDHK activity may be effective for increasing glucose utilization in diabetes treatment Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.2 AZD7545 noncompetitive to ATP Homo sapiens
2.7.11.2 AZD7545 noncompetitive to ATP, IC50 values for isozymes PDHK1, PDHK2, and PDHK4 Rattus norvegicus
2.7.11.2 compound K noncompetitive to ATP, IC50 values for isozymes PDHK1, PDHK2, and PDHK4 Rattus norvegicus
2.7.11.2 Dichloroacetate noncompetitive to ATP Rattus norvegicus
2.7.11.2 additional information isozyme-specific inhibition by AZD7545 analogues Rattus norvegicus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.2 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
-
 ?
2.7.11.2 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

EC Number Organism UniProt Comment Textmining
2.7.11.2 Homo sapiens
-
 isozymes PDHK1, PDHK2, PDHK3, and PDHK4
-
2.7.11.2 Rattus norvegicus
-
 Wistar rats, isozymes PDHK1, PDHK2, PDHK3, and PDHK4
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.2 heart
-
 Rattus norvegicus
-
2.7.11.2 kidney
-
 Rattus norvegicus
-
2.7.11.2 liver
-
 Rattus norvegicus
-
2.7.11.2 additional information tissue-specific isozyme distribution Homo sapiens
-
2.7.11.2 additional information tissue-specific isozyme distribution Rattus norvegicus
-
2.7.11.2 pancreatic beta cell
-
 Homo sapiens
-
2.7.11.2 pancreatic beta cell
-
 Rattus norvegicus
-
2.7.11.2 skeletal muscle
-
 Homo sapiens
-
2.7.11.2 skeletal muscle
-
 Rattus norvegicus
-
2.7.11.2 tibialis anterior
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

EC Number Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
2.7.11.2 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)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.2 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
-
 ?
2.7.11.2 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
-
 ?
2.7.11.2 ATP + pyruvate dehydrogenase phosphorylation of 3 serine residues of the E2 domain, isozyme-specific activity Homo sapiens ADP + phosphorylated pyruvate dehydrogenase
-
 ?
2.7.11.2 ATP + pyruvate dehydrogenase phosphorylation of 3 serine residues of the E2 domain, isozyme-specific activity Rattus norvegicus ADP + phosphorylated pyruvate dehydrogenase
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.2 PDH kinase
-
 Homo sapiens
2.7.11.2 PDH kinase
-
 Rattus norvegicus
2.7.11.2 PDHK
-
 Homo sapiens
2.7.11.2 PDHK
-
 Rattus norvegicus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.2 30
-
 assay at Rattus norvegicus

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.2 ATP
-
 Homo sapiens
2.7.11.2 ATP
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.2 0.2
-
 Dichloroacetate isozyme PDHK2, 30°C Rattus norvegicus
2.7.11.2 0.5
-
 Dichloroacetate isozyme PDHK4, 30°C Rattus norvegicus
2.7.11.2 1
-
 Dichloroacetate isozyme PDHK1, 30°C Rattus norvegicus