Proteins > [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial
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[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial
A [pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15119]
Synonyms
EC 2.7.11.2;
Pyruvate dehydrogenase kinase isoform 2;
PDH kinase 2;
PDKII
Research
Bioassay Publications (12)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (16.67) | 18.2507 |
| 2000's | 1 (8.33) | 29.6817 |
| 2010's | 8 (66.67) | 24.3611 |
| 2020's | 1 (8.33) | 2.80 |
Compounds (11)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
[no title available]Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Identification of pyruvate dehydrogenase kinase 1 inhibitors with anti-osteosarcoma activity.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 27, Issue:24, 2017
Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.The Journal of biological chemistry, , Feb-14, Volume: 289, Issue:7, 2014
Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK).Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 9, Issue:15, 1999
Anilides of (R)-trifluoro-2-hydroxy-2-methylpropionic acid as inhibitors of pyruvate dehydrogenase kinase.Journal of medicinal chemistry, , Jun-01, Volume: 43, Issue:11, 2000
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.Journal of medicinal chemistry, , Jul-29, Volume: 42, Issue:15, 1999
[no title available]Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity.European journal of medicinal chemistry, , Feb-15, Volume: 164, 2019
Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia.MedChemComm, , Nov-01, Volume: 9, Issue:11, 2018
Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.Journal of medicinal chemistry, , 03-23, Volume: 60, Issue:6, 2017
Enables
This protein enables 5 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] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| 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] |
| 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] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
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] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| pyruvate dehydrogenase complex | cellular component | A multi-enzyme complex that catalyzes the oxidative decarboxylation of pyruvate to form acetyl-CoA. The complex comprises multiple copies of three enzymes referred to as E1, E2 and E3: pyruvate dehydrogenase (E1, which may be a homodimer or a heterotetramer of two alpha and two beta subunits, depending on species), dihydrolipoamide S-acetyltransferase (E2), and dihydrolipoamide dehydrogenase (E3). Additional proteins may also be present. [PMID:36863425] |
Involved In
This protein is involved in 13 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] |
| regulation of gluconeogenesis | biological process | Any process that modulates the frequency, rate or extent of gluconeogenesis, the formation of glucose from noncarbohydrate precursors, such as pyruvate, amino acids and glycerol. [GOC:go_curators] |
| regulation of pH | biological process | Any process involved in the maintenance of an internal equilibrium of hydrogen ions, thereby modulating the internal pH, within an organism or cell. [GOC:dph, GOC:go_curators, GOC:tb] |
| insulin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of the insulin receptor binding to insulin. [GOC:ceb] |
| 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 cellular ketone metabolic process | biological process | Any process that modulates the chemical reactions and pathways involving any of a class of organic compounds that contain the carbonyl group, CO, and in which the carbonyl group is bonded only to carbon atoms. The general formula for a ketone is RCOR, where R and R are alkyl or aryl groups. [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] |
| cellular response to nutrient | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nutrient stimulus. [GOC:mah] |
| cellular response to reactive oxygen species | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a reactive oxygen species stimulus. Reactive oxygen species include singlet oxygen, superoxide, and oxygen free radicals. [GOC:mah] |
| glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
| regulation of calcium-mediated signaling | biological process | Any process that modulates the frequency, rate or extent of calcium-mediated signaling, the process in which a cell uses calcium ions to convert an extracellular signal into a response. [GOC:ai] |
| intrinsic apoptotic signaling pathway by p53 class mediator | 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 by the cell cycle regulator phosphoprotein p53, or an equivalent protein, and ends when the execution phase of apoptosis is triggered. [GOC:mah, GOC:mtg_apoptosis] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |