Proteins > [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
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[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
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
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Discovery of novel pyruvate dehydrogenase kinases inhibitors by screening of an in-house small molecule library for anti-lung cancer therapeutics.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 29, Issue:2, 2019
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation.Journal of medicinal chemistry, , Apr-14, Volume: 59, Issue:7, 2016
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
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
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
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.Journal of medicinal chemistry, , Jul-29, Volume: 47, Issue:16, 2004
Structure-based drug design of novel and highly potent pyruvate dehydrogenase kinase inhibitors.Bioorganic & medicinal chemistry, , 12-15, Volume: 52, 2021
[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
[no title available],
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] |