Proteins > [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial
Page last updated: 2024-08-07 13:33:11
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial
A [pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q15120]
Synonyms
EC 2.7.11.2;
Pyruvate dehydrogenase kinase isoform 3
Research
Bioassay Publications (10)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (20.00) | 18.2507 |
| 2000's | 1 (10.00) | 29.6817 |
| 2010's | 7 (70.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (9)
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
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
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
[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] |
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| 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 3 target(s):
| Target | Category | Definition |
|---|
| nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
| 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] |
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 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| peptidyl-serine phosphorylation | biological process | The phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037] |
| peroxisome proliferator activated receptor signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to any of the peroxisome proliferator activated receptors (alpha, beta or gamma) in the nuclear membrane, and ending with the initiation or termination of the transcription of target genes. [GOC:BHF, PMID:18221086] |
| 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] |
| 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] |
| regulation of reactive oxygen species metabolic process | biological process | Any process that modulates the frequency, rate or extent of reactive oxygen species metabolic process. [GOC:mah] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |