TARGETID

T15776

UNIPROID

PDK1_HUMAN

TARGNAME

Pyruvate dehydrogenase kinase 1 (PDHK1)

GENENAME

PDK1

TARGTYPE

Clinical trial target

SYNONYMS

Pyruvate dehydrogenase kinase isoform 1; Pyruvate dehydrogenase (acetyl-transferring) kinase isozyme 1, mitochondrial; PDHK1; PDH kinase 1

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.

PDBSTRUC

2Q8H; 2Q8G; 2Q8F

BIOCLASS

Kinase

ECNUMBER

EC 2.7.11.2

SEQUENCE

MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMKQFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQELLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYFLDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLCDLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPPIQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLPISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDWCVPSREPKDMTTFRSA

DRUGINFO

Dichloroacetate

DRUGINFO

1,2-dihydroindazolo[4,3-bc][1,5]benzoxazepine derivative 1

DRUGINFO

Benzimidazole and imidazopyridine derivative 1

DRUGINFO

Benzonaphthyridine derivative 1

DRUGINFO

Benzonaphthyridine derivative 2

DRUGINFO

Bis-indolylmaleimide derivative 1

DRUGINFO

Dibenzo [c,f]-[2,7]naphthyridine derivative 1

DRUGINFO

Heteroaryl-carboxamide derivative 1

DRUGINFO

Heteroaryl-carboxamide derivative 10