Page last updated: 2024-08-07 17:08:49
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
A [pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15118]
Synonyms
EC 2.7.11.2;
Pyruvate dehydrogenase kinase isoform 1;
PDH kinase 1
Research
Bioassay Publications (31)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (6.45) | 18.2507 |
| 2000's | 9 (29.03) | 29.6817 |
| 2010's | 18 (58.06) | 24.3611 |
| 2020's | 2 (6.45) | 2.80 |
Compounds (29)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| nu6102 | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| dichloroacetic acid | Homo sapiens (human) | IC50 | 1,677.6000 | 4 | 5 |
| dibenzothiazyl disulfide | Homo sapiens (human) | IC50 | 0.3790 | 1 | 1 |
| nandrolone | Homo sapiens (human) | IC50 | 120.0000 | 1 | 1 |
| abietic acid | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| staurosporine | Homo sapiens (human) | IC50 | 0.0005 | 2 | 2 |
| dehydroabietylamine | Homo sapiens (human) | IC50 | 9.5000 | 1 | 1 |
| birb 796 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
| zeneca zd 6169 | Homo sapiens (human) | IC50 | 9.3000 | 1 | 1 |
| 6-bromoindirubin-3'-oxime | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| sodium dichloroacetate | Homo sapiens (human) | IC50 | 1,000.0000 | 2 | 2 |
| monorden | Homo sapiens (human) | IC50 | 235.9333 | 3 | 3 |
| norethisterone-3-oxime | Homo sapiens (human) | IC50 | 5.8000 | 1 | 1 |
| tofacitinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ly2090314 | Homo sapiens (human) | IC50 | 6.2000 | 1 | 1 |
| bx795 | Homo sapiens (human) | IC50 | 0.0650 | 1 | 1 |
| sotrastaurin | Homo sapiens (human) | IC50 | 6.7000 | 1 | 1 |
| l 783277 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| at 7519 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-[2-(2-chloro-4-fluoroanilino)-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pha 767491 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd 7545 | Homo sapiens (human) | IC50 | 0.0410 | 1 | 1 |
| mrt67307 | Homo sapiens (human) | IC50 | 0.4210 | 1 | 1 |
| pha 793887 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| gsk 2334470 | Homo sapiens (human) | IC50 | 0.0025 | 1 | 0 |
| nms p937 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| ver-246608 | Homo sapiens (human) | IC50 | 0.1258 | 7 | 6 |
| ver-246608 | Homo sapiens (human) | Ki | 0.0280 | 1 | 1 |
| at 9283 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| nms-e973 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|---|---|---|---|---|
| zeneca zd 6169 | Homo sapiens (human) | EC50 | 8.3000 | 1 | 1 |
| sodium dichloroacetate | Homo sapiens (human) | EC50 | 2,915.0000 | 2 | 2 |
| sodium dichloroacetate | Homo sapiens (human) | Kd | 1,000.0000 | 1 | 1 |
| ver-246608 | Homo sapiens (human) | Kd | 0.1500 | 1 | 1 |
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|---|---|
| protein kinase activity | molecular function | Catalysis of the phosphorylation of an amino acid residue in a protein, usually according to the reaction: a protein + ATP = a phosphoprotein + ADP. [PMID:25399640] |
| pyruvate dehydrogenase (acetyl-transferring) kinase activity | molecular function | Catalysis of the reaction: ATP + pyruvate dehydrogenase (acetyl-transferring) = ADP + pyruvate dehydrogenase (acetyl-transferring) phosphate. [EC:2.7.11.2] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| mitochondrial matrix | cellular component | The gel-like material, with considerable fine structure, that lies in the matrix space, or lumen, of a mitochondrion. It contains the enzymes of the tricarboxylic acid cycle and, in some organisms, the enzymes concerned with fatty acid oxidation. [GOC:as, ISBN:0198506732] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|---|---|
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|---|---|
| glucose metabolic process | biological process | The chemical reactions and pathways involving glucose, the aldohexose gluco-hexose. D-glucose is dextrorotatory and is sometimes known as dextrose; it is an important source of energy for living organisms and is found free as well as combined in homo- and hetero-oligosaccharides and polysaccharides. [ISBN:0198506732] |
| cell population proliferation | biological process | The multiplication or reproduction of cells, resulting in the expansion of a cell population. [GOC:mah, GOC:mb] |
| intrinsic apoptotic signaling pathway in response to oxidative stress | biological process | The series of molecular signals in which an intracellular signal is conveyed to trigger the apoptotic death of a cell. The pathway is induced in response to oxidative stress, a state often resulting from exposure to high levels of reactive oxygen species, and ends when the execution phase of apoptosis is triggered. [GOC:ai, GOC:mtg_apoptosis] |
| regulation of acetyl-CoA biosynthetic process from pyruvate | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of acetyl-CoA from pyruvate. [GOC:dph, GOC:tb] |
| regulation of glucose metabolic process | biological process | Any process that modulates the rate, frequency or extent of glucose metabolism. Glucose metabolic processes are the chemical reactions and pathways involving glucose, the aldohexose gluco-hexose. [GOC:BHF, GOC:tb] |
| hypoxia-inducible factor-1alpha signaling pathway | biological process | The series of molecular signals mediated by hypoxia-inducible factor (HIF1) in response to lowered oxygen levels (hypoxia). Under hypoxic conditions, the oxygen-sensitive alpha-subunit of hypoxia-inducible factor (HIF)-1 dimerizes with a HIF1-beta subunit (also called ARNT or aryl-hydrocarbon-receptor nuclear translocator), translocates to the nucleus and activates transcription of genes whose products participate in responding to hypoxia. [GOC:bf, GOC:jc, http://www.sabiosciences.com/pathway.php?sn=HIF1Alpha_Pathway] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |