Application | Comment | Organism |
---|---|---|
medicine | the results implicate the invariant C-terminal DW-motif anchoring site as a drug target for the inhibition of aberrant PDK activity in cancer and diabetes | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
wild-type and variant human PDK2 proteins are expressed as N-terminal His6-tagged SUMO fusions | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
D382A/W383A | substitutions in the DW-motif | Homo sapiens |
R149A | substitution of an interacting residue of the DW-motif, mutant shows drastic increase in apparent IC50 value for dichloroacetate, increased affinity for ADP and ATP | Homo sapiens |
Y145F | substitution of an interacting residue of the DW-motif, increased affinity for ADP and ATP | Homo sapiens |
Y145F/R149A | mutant shows drastic increase in apparent IC50 value for dichloroacetate | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Dichloroacetate | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [pyruvate dehydrogenase (acetyl-transferring)] | Homo sapiens | - |
ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
with nickel-nitrilotriacetic acid resin and subsequently on a Superdex S200 column | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + [pyruvate dehydrogenase (acetyl-transferring)] | - |
Homo sapiens | ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate | - |
? |
Subunits | Comment | Organism |
---|---|---|
homodimer | - |
Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
PDK2 | - |
Homo sapiens |
pyruvate dehydrogenase kinase 2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
23 | - |
activity assay | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
activity assay | Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.29 | - |
wild-type enzyme, apparent IC50 for basal activity | Homo sapiens | Dichloroacetate | |
0.48 | - |
wild-type enzyme, apparent IC50 for E2p/E3BP-dependent activity | Homo sapiens | Dichloroacetate | |
3.04 | - |
mutant Y145F, apparent IC50 for basal activity | Homo sapiens | Dichloroacetate | |
3.24 | - |
mutant Y145F, apparent IC50 for E2p/E3BP-dependent activity | Homo sapiens | Dichloroacetate | |
35.3 | - |
mutant D382A/W383A, apparent IC50 for E2p/E3BP-dependent activity | Homo sapiens | Dichloroacetate | |
37.9 | - |
mutant D382A/W383A, apparent IC50 for basal activity | Homo sapiens | Dichloroacetate | |
86.3 | - |
mutant Y145F/R149A, apparent IC50 for E2p/E3BP-dependent activity | Homo sapiens | Dichloroacetate | |
98.7 | - |
mutant R149A, apparent IC50 for basal activity | Homo sapiens | Dichloroacetate | |
102 | - |
mutant Y145F/R149A, apparent IC50 for basal activity | Homo sapiens | Dichloroacetate | |
108 | - |
mutant R149A, apparent IC50 for E2p/E3BP-dependent activity | Homo sapiens | Dichloroacetate |
General Information | Comment | Organism |
---|---|---|
physiological function | the mitochondrial pyruvate dehydrogenase complex, PDC, is down-regulated by phosphorylation catalyzed by pyruvate dehydrogenase kinase isoforms | Homo sapiens |