Activating Compound | Comment | Organism | Structure |
---|---|---|---|
acetyl-CoA | stimulation by acetyl-CoA requires both K+ and at least one anion, phosphate or chloride, mechanisms for stimulation of PDK2, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overview | Homo sapiens | |
acetyl-CoA | stimulation by acetyl-CoA requires both K+ and at least one anion, phosphate or chloride, mechanisms for stimulation of PDK2, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overview | Rattus norvegicus | |
NADH | stimulation by NADH requires both K+ and at least one anion, phosphate or chloride, mechanisms for stimulation of PDK2, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overview | Homo sapiens | |
NADH | stimulation by NADH requires both K+ and at least one anion, phosphate or chloride, mechanisms for stimulation of PDK2, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overview | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
ADP | - |
Homo sapiens | |
ADP | - |
Rattus norvegicus | |
AZD7545 | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor | Homo sapiens | |
AZD7545 | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor | Rattus norvegicus | |
compound K | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor | Homo sapiens | |
compound K | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor | Rattus norvegicus | |
additional information | PDK2 inhibition mechanism, overview | Homo sapiens | |
additional information | PDK2 inhibition mechanism, overview | Rattus norvegicus | |
Nov3r | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor, a mimic of the acetyl-dihydrolipoyl group, inhibits PDK2 | Homo sapiens | |
Nov3r | an amide of trifluoro-2-hydroxy-2-methylpropionic acid, a tight binding inhibitor, a mimic of the acetyl-dihydrolipoyl group, inhibits PDK2 | Rattus norvegicus | |
pyruvate | - |
Homo sapiens | |
pyruvate | - |
Rattus norvegicus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
mitochondrion | - |
Homo sapiens | 5739 | - |
mitochondrion | - |
Rattus norvegicus | 5739 | - |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Cl- | activates | Homo sapiens | |
Cl- | activates | Rattus norvegicus | |
K+ | activates, the Km for ATP is decreased and ADP inhibition is enhanced by elevating K+ ion levels, ligand-induced changes in K+ binding, overview | Homo sapiens | |
K+ | activates, the Km for ATP is decreased and ADP inhibition is enhanced by elevating K+ ion levels, ligand-induced changes in K+ binding, overview | Rattus norvegicus | |
Mg2+ | activates | Homo sapiens | |
Mg2+ | activates | Rattus norvegicus | |
phosphate | activates | Homo sapiens | |
phosphate | activates | Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | PDC activation also triggers apoptosis in cancer cells that selectively convert glucose to lactate, regulation of the pyruvate dehydrogenase complex, PDK4 overexpression in association with type I diabetes | ? | - |
? | |
additional information | Rattus norvegicus | PDC activation also triggers apoptosis in cancer cells that selectively convert glucose to lactate, regulation of the pyruvate dehydrogenase complex, PDK4 overexpression in association with type I diabetes | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
adipose tissue | mainly isozyme PDK2 | Homo sapiens | - |
adipose tissue | mainly isozyme PDK2 | Rattus norvegicus | - |
heart | - |
Homo sapiens | - |
heart | - |
Rattus norvegicus | - |
liver | isozymes PDK2 and PDK4 | Homo sapiens | - |
liver | isozymes PDK2 and PDK4, obese Zucker rats show levels of expression of PDK2 and PDK4 in liver and skeletal muscle similar to those found in lean rats | Rattus norvegicus | - |
skeletal muscle | isozymes PDK2 and PDK4 | Homo sapiens | - |
skeletal muscle | isozymes PDK2 and PDK4, obese Zucker rats show levels of expression of PDK2 and PDK4 in liver and skeletal muscle similar to those found in lean rats | Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | PDC activation also triggers apoptosis in cancer cells that selectively convert glucose to lactate, regulation of the pyruvate dehydrogenase complex, PDK4 overexpression in association with type I diabetes | Homo sapiens | ? | - |
? | |
additional information | PDC activation also triggers apoptosis in cancer cells that selectively convert glucose to lactate, regulation of the pyruvate dehydrogenase complex, PDK4 overexpression in association with type I diabetes | Rattus norvegicus | ? | - |
? | |
additional information | PD kinase isozymes PDK1, PDK2, PDK3 and PDK4, reduce the active form of pyruvate dehydrogenase complex, PDC, via binding to the inner lipoyl domain L2 of the dihydrolipoyl acetyltransferase E2, PDK rapidly access their E2-bound PD substrate. The E2-enhanced activity of the widely distributed PDK2 is limited by dissociation of ADP from its C-terminal catalytic domain, and this is further slowed by pyruvate binding to the N-terminal regulatory domain, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overall reaction of the pyruvate dehydrogenase complex, overview | Homo sapiens | ? | - |
? | |
additional information | PD kinase isozymes PDK1, PDK2, PDK3 and PDK4, reduce the active form of pyruvate dehydrogenase complex, PDC, via binding to the inner lipoyl domain L2 of the dihydrolipoyl acetyltransferase E2, PDK rapidly access their E2-bound PD substrate. The E2-enhanced activity of the widely distributed PDK2 is limited by dissociation of ADP from its C-terminal catalytic domain, and this is further slowed by pyruvate binding to the N-terminal regulatory domain, via the reverse of the PDC reaction, NADH and acetyl-CoA reductively acetylate lipoyl group of L2, which binds to the R domain and stimulates PDK2 activity by speeding up ADP dissociation, overall reaction of the pyruvate dehydrogenase complex, overview | Rattus norvegicus | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
More | components and organization of the mammalian pyruvate dehydrogenase complex, including the enzyme | Homo sapiens |
More | components and organization of the mammalian pyruvate dehydrogenase complex, including the enzyme | Rattus norvegicus |
Synonyms | Comment | Organism |
---|---|---|
PDK2 | - |
Homo sapiens |
PDK2 | - |
Rattus norvegicus |
PDK4 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens | |
ATP | - |
Rattus norvegicus |