Tchem PDK2 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial

Protein Summary

Description

Kinase that plays a key role in the regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis. This gene encodes a member of the pyruvate dehydrogenase kinase family. The encoded protein phosphorylates pyruvate dehydrogenase, down-regulating the activity of the mitochondrial pyruvate dehydrogenase complex. Overexpression of this gene may play a role in both cancer and diabetes. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene. [provided by RefSeq, Dec 2010]

Uniprot Accession IDs

• Q15119
• A8K3A7
• B3KNW0
• Q6P515
• Q9BS05

Gene Name

• PDK2

Ensembl ID

• ENST00000007708
• ENSP00000007708
• ENSG00000005882
• ENST00000503176
• ENSP00000420927
• ENST00000614357
• ENSP00000481915

Symbol

• PDHK2
• PDHK2
• PDKII

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
molecular function	0.95
virus perturbation	0.72
kinase perturbation	0.71
biological process	0.69
tissue	0.68

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 2, Mitochondrial

DTO Classes

Protein / Kinase / Protein Kinase / Atypical Group / Pdhk Family / Pdhk Subfamily / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 2, Mitochondrial

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 147.65   (req: < 5)

Gene RIFs: 33   (req: <= 3)

Antibodies: 496   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 147.65   (req: >= 5)

Gene RIFs: 33   (req: > 3)

Antibodies: 496   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 16

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 86

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0