Names & Taxonomy
- Uniprot ID:
- Q15118
- Entry Name:
- PDK1_HUMAN
- Status:
- reviewed
- Protein Names:
- [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (EC 2.7.11.2) (Pyruvate dehydrogenase kinase isoform 1) (PDH kinase 1)
- Gene Names:
- PDK1 PDHK1
- Gene Names Primary:
- PDK1
- Organism:
- Homo sapiens (Human)
Structure
- Length:
- 436
- Sequence:
- MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMKQFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQELLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYFLDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLCDLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPPIQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLPISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDWCVPSREPKDMTTFRSA
- Proteomes:
- UP000005640
Subcellular location
- Subcellular Location:
- Mitochondrion matrix
Function
- Function:
- 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.
- Catalytic Activity:
- ATP + = ADP + phosphate.
- Enzyme Regulation:
- ENZYME REGULATION: Activity is enhanced by binding to the pyruvate dehydrogenase subunit DLAT. Inhibited by AZD7545; this compound interferes with DLAT binding and thereby inhibits kinase activity. Inhibited by dichloroacetate and radicicol.
- Gene Ontology Go:
- mitochondrial matrix
mitochondrial pyruvate dehydrogenase complex
mitochondrion
ATP binding
protein kinase activity
pyruvate dehydrogenase (acetyl-transferring) kinase activity
cell proliferation
cellular metabolic process
glucose metabolic process
hypoxia-inducible factor-1alpha signaling pathway
intrinsic apoptotic signaling pathway in response to oxidative stress
mitophagy in response to mitochondrial depolarization
protein phosphorylation
pyruvate metabolic process
regulation of acetyl-CoA biosynthetic process from pyruvate
regulation of glucose metabolic process
small molecule metabolic process - Gene Ontology Biological Process:
- cell proliferation
cellular metabolic process
glucose metabolic process
hypoxia-inducible factor-1alpha signaling pathway
intrinsic apoptotic signaling pathway in response to oxidative stress
mitophagy in response to mitochondrial depolarization
protein phosphorylation
pyruvate metabolic process
regulation of acetyl-CoA biosynthetic process from pyruvate
regulation of glucose metabolic process
small molecule metabolic process - Gene Ontology Molecular Function:
- ATP binding
protein kinase activity
pyruvate dehydrogenase (acetyl-transferring) kinase activity - Gene Ontology Cellular Component:
- mitochondrial matrix
mitochondrial pyruvate dehydrogenase complex
mitochondrion - Keywords:
- 3D-structure
ATP-binding
Alternative splicing
Carbohydrate metabolism
Complete proteome
Glucose metabolism
Kinase
Mitochondrion
Nucleotide-binding
Phosphoprotein
Polymorphism
Reference proteome
Transferase
Transit peptide - Interacts With:
- Q16513