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. Multiple alternatively spliced transcript variants have been found for this gene. [provided by RefSeq, Jun 2013]

Uniprot Accession IDs

• Q15118
• B2R6T1
• B7Z937
• D3DPD8
• E9PD65
• Q308M4

Gene Name

• PDK1

Ensembl ID

• ENST00000282077
• ENSP00000282077
• ENSG00000152256
• ENST00000392571
• ENSP00000376352
• ENST00000410055
• ENSP00000386985

Symbol

• PDHK1

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

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Protein Kinase / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 1, Mitochondrial

DTO Classes

Protein / Kinase / Protein Kinase / Atypical Group / Pdhk Family / [Pyruvate Dehydrogenase (Acetyl-transferring)] Kinase Isozyme 1, 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: 154.44   (req: < 5)

Gene RIFs: 69   (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: 69   (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