Proteins > [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial
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[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial
A [pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q16654]
Synonyms
EC 2.7.11.2;
Pyruvate dehydrogenase kinase isoform 4
Research
Bioassay Publications (11)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (18.18) | 18.2507 |
| 2000's | 2 (18.18) | 29.6817 |
| 2010's | 6 (54.55) | 24.3611 |
| 2020's | 1 (9.09) | 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
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
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
[no title available]Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 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 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 15 target(s):
| Target | Category | Definition |
|---|
| 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] |
| cellular response to starvation | 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 deprivation of nourishment. [GOC:jl] |
| 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] |
| regulation of fatty acid biosynthetic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of fatty acids, any of the aliphatic monocarboxylic acids that can be liberated by hydrolysis from naturally occurring fats and oils. [GOC:go_curators, GOC:jl] |
| 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] |
| response to starvation | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a starvation stimulus, deprivation of nourishment. [GOC:go_curators] |
| regulation of bone resorption | biological process | Any process that modulates the frequency, rate or extent of bone tissue loss (resorption). [GOC:ai] |
| regulation of fatty acid oxidation | biological process | Any process that modulates the frequency, rate or extent of fatty acid oxidation. [GOC:ai] |
| cellular response to fatty acid | 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 fatty acid stimulus. [GOC:mah] |
| reactive oxygen species metabolic process | biological process | The chemical reactions and pathways involving a reactive oxygen species, any molecules or ions formed by the incomplete one-electron reduction of oxygen. They contribute to the microbicidal activity of phagocytes, regulation of signal transduction and gene expression, and the oxidative damage to biopolymers. [GOC:mah] |
| negative regulation of anoikis | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of anoikis. [GOC:obol] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |