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Tchem
PDK1
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial

Protein Summary
Description
Kinase that plays a key role in 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. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress. Pyruvate dehydrogenase (PDH) is a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDK) results in inactivation. ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000282077
  • ENSP00000282077
  • ENSG00000152256
  • ENST00000392571
  • ENSP00000376352
  • ENST00000410055
  • ENSP00000386985

Symbol
  • PDHK1
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
transcription factor perturbation
0.98
PubMedID
0.94
kinase perturbation
0.91
molecular function
0.91
transcription factor binding site profile
0.88


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: 154.44   (req: < 5)
Gene RIFs: 36   (req: <= 3)
Antibodies: 636   (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: 154.44   (req: >= 5)
Gene RIFs: 36   (req: > 3)
Antibodies: 636   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 9
Tchem

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

Active Ligands: 119
Tclin

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

Active Drug: 0