Page last updated: 2024-08-07 23:19:04

Pyruvate kinase PKM

A pyruvate kinase PKM that is encoded in the genome of human. [PRO:DNx, UniProtKB:P14618]

Synonyms

EC 2.7.1.40;
Cytosolic thyroid hormone-binding protein;
CTHBP;
Opa-interacting protein 3;
OIP-3;
Pyruvate kinase 2/3;
Pyruvate kinase muscle isozyme;
Thyroid hormone-binding protein 1;
THBP1;
Tumor M2-PK;
p58

Research

Bioassay Publications (11)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (72.73)24.3611
2020's3 (27.27)2.80

Compounds (63)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
spermidineHomo sapiens (human)IC501.410011
indoprofenHomo sapiens (human)IC5021.000011
vitamin k 3Homo sapiens (human)IC50150.000011
nalidixic acidHomo sapiens (human)IC5053.000011
gliotoxinHomo sapiens (human)IC5022.640011
vitamin k5Homo sapiens (human)IC5028.000011
hematoxylinHomo sapiens (human)IC50340.000011
syringic acidHomo sapiens (human)IC5013.800011
3-hydroxyflavoneHomo sapiens (human)IC501.750011
3-hydroxyflavoneHomo sapiens (human)Ki3.530011
5-hydroxyflavoneHomo sapiens (human)IC501.390011
5-hydroxyflavoneHomo sapiens (human)Ki3.530011
epicatechinHomo sapiens (human)IC501.330011
6-hydroxyflavoneHomo sapiens (human)IC501.240011
6-hydroxyflavoneHomo sapiens (human)Ki3.530011
alkanninHomo sapiens (human)IC500.900022
neoeriocitrinHomo sapiens (human)IC500.650011
oxymatrineHomo sapiens (human)IC505.000011
tanshinone ii aHomo sapiens (human)IC501,920.000011
taxifolinHomo sapiens (human)IC501.160011
ferulic acidHomo sapiens (human)IC5011.400011
shikoninHomo sapiens (human)IC507.960088
apigeninHomo sapiens (human)IC500.990022
fisetinHomo sapiens (human)IC500.900011
scutellareinHomo sapiens (human)IC5041.666733
wogoninHomo sapiens (human)IC502.010011
wogoninHomo sapiens (human)Ki3.530011
polydatinHomo sapiens (human)IC50128.000011
7-hydroxyflavoneHomo sapiens (human)IC502.120011
7-hydroxyflavoneHomo sapiens (human)Ki3.530011
(-)-catechin-3-O-gallateHomo sapiens (human)IC500.850011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
serineHomo sapiens (human)EC501,300.000011
fructose-1,6-diphosphateHomo sapiens (human)EC500.023011
micheliolideHomo sapiens (human)EC500.006011
6-[(2-fluorophenyl)methyl]-2,4-dimethyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)EC500.038011
N-(4-methylphenyl)-2-oxo-3,4-dihydro-1H-quinoline-6-sulfonamideHomo sapiens (human)EC501.400011
N-(3,4-dimethylphenyl)-2-oxo-3,4-dihydro-1H-quinoline-6-sulfonamideHomo sapiens (human)EC500.790011
quercetin 3-o-glucopyranosideHomo sapiens (human)EC500.001311
myricetinHomo sapiens (human)EC500.000511
N-(3-methylphenyl)-2-oxo-3,4-dihydro-1H-quinoline-6-sulfonamideHomo sapiens (human)EC500.250011
N-(4-fluorophenyl)-2-oxo-3,4-dihydro-1H-quinoline-6-sulfonamideHomo sapiens (human)EC506.000011
6-[(3-methoxyphenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)EC500.073011
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)EC500.092022
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]anilineHomo sapiens (human)EC500.038033

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
alpha-D-fructofuranose 1,6-bisphosphateHomo sapiens (human)Activity0.080011
alpha-D-fructofuranose 1,6-bisphosphateHomo sapiens (human)Km100.000022
1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-4-(4-methoxyphenyl)sulfonylpiperazineHomo sapiens (human)AC500.430522
6-[(2-fluorophenyl)methyl]-2,4-dimethyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)AC500.194522
6-[(2-fluorophenyl)methyl]-2,4-dimethyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)Km115.000022
1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-4-(4-fluorophenyl)sulfonylpiperazineHomo sapiens (human)AC500.094011
(2R)-4-(2,6-difluorophenyl)sulfonyl-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazineHomo sapiens (human)AC503.100011
(2R)-1-(2,6-difluorophenyl)sulfonyl-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazineHomo sapiens (human)AC502.930011
(2S)-4-(2,6-difluorophenyl)sulfonyl-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazineHomo sapiens (human)AC504.340011
(2S)-1-(2,6-difluorophenyl)sulfonyl-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-2-methylpiperazineHomo sapiens (human)AC509.180011
4-(2,6-difluorophenyl)sulfonyl-1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)piperidineHomo sapiens (human)AC500.254011
1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-4-(2-pyridinylsulfonyl)piperazineHomo sapiens (human)AC500.542011
N-[1-(2,6-difluorophenyl)sulfonyl-4-piperidinyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC509.000011
1-(2,6-difluorophenyl)sulfonyl-4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepaneHomo sapiens (human)AC500.866011
N-[4-[(2,6-difluorophenyl)sulfonylamino]cyclohexyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC5018.555012
1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-4-[3-(trifluoromethyl)phenyl]sulfonylpiperazineHomo sapiens (human)AC500.209011
N-[[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-azetidinyl]methyl]-2,6-difluorobenzenesulfonamideHomo sapiens (human)AC504.470011
N-[[1-(2,6-difluorophenyl)sulfonyl-3-azetidinyl]methyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC503.050011
N-[1-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-3-pyrrolidinyl]-2,6-difluorobenzenesulfonamideHomo sapiens (human)AC5015.000011
N-[3-[(2,6-difluorophenyl)sulfonylamino]propyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC503.850011
N-[5-[(2,6-difluorophenyl)sulfonylamino]pentyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC502.330011
N-[6-[(2,6-difluorophenyl)sulfonylamino]hexyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC504.830011
N-[2-[(2,6-difluorophenyl)sulfonylamino]ethyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC5015.000011
N-[1-(2,6-difluorophenyl)sulfonyl-3-pyrrolidinyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC5010.000011
N-[4-[(2,6-difluorophenyl)sulfonylamino]butyl]-2,3-dihydro-1,4-benzodioxin-6-sulfonamideHomo sapiens (human)AC507.970011
3-[(2-fluorophenyl)methyl]-5-methyl-4-thieno[3,4]pyrrolo[1,3-d]pyrimidinoneHomo sapiens (human)AC5035.000011
6-[(2-fluorophenyl)methyl]-2-(1-hydroxyethyl)-4-methyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)AC500.136011
6-[(3-methoxyphenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)AC500.073011
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)AC500.092022
6-[(3-aminophenyl)methyl]-4-methyl-2-methylsulfinyl-5-thieno[3,4]pyrrolo[1,3-d]pyridazinoneHomo sapiens (human)EC900.470011
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]anilineHomo sapiens (human)AC500.045022
3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylsulfonyl)-1,4-diazepan-1-yl]sulfonyl]anilineHomo sapiens (human)EC900.680011

Enables

This protein enables 10 target(s):

TargetCategoryDefinition
magnesium ion bindingmolecular functionBinding to a magnesium (Mg) ion. [GOC:ai]
RNA bindingmolecular functionBinding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah]
mRNA bindingmolecular functionBinding to messenger RNA (mRNA), an intermediate molecule between DNA and protein. mRNA includes UTR and coding sequences, but does not contain introns. [GOC:kmv, GOC:pr, SO:0000234]
protein tyrosine kinase activitymolecular functionCatalysis of the reaction: ATP + a protein tyrosine = ADP + protein tyrosine phosphate. [RHEA:10596]
pyruvate kinase activitymolecular functionCatalysis of the reaction: = ADP + H+ + phosphoenolpyruvate => ATP + pyruvate. [EC:2.7.1.40, RHEA:18159]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
ATP bindingmolecular functionBinding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732]
MHC class II protein complex bindingmolecular functionBinding to a class II major histocompatibility complex. [GOC:mtg_signal, GOC:vw]
potassium ion bindingmolecular functionBinding to a potassium ion (K+). [GOC:mah]
cadherin bindingmolecular functionBinding to cadherin, a type I membrane protein involved in cell adhesion. [GOC:bf]

Located In

This protein is located in 13 target(s):

TargetCategoryDefinition
extracellular regioncellular componentThe space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators]
nucleuscellular componentA membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
mitochondrioncellular componentA 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]
rough endoplasmic reticulumcellular componentThe rough (or granular) endoplasmic reticulum (ER) has ribosomes adhering to the outer surface; the ribosomes are the site of translation of the mRNA for those proteins which are either to be retained within the cisternae (ER-resident proteins), the proteins of the lysosomes, or the proteins destined for export from the cell. Glycoproteins undergo their initial glycosylation within the cisternae. [ISBN:0198506732]
cytosolcellular componentThe part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
ciliumcellular componentA specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface and of some cytoplasmic parts. Each cilium is largely bounded by an extrusion of the cytoplasmic (plasma) membrane, and contains a regular longitudinal array of microtubules, anchored to a basal body. [GOC:cilia, GOC:curators, GOC:kmv, GOC:vw, ISBN:0198547684, PMID:16824949, PMID:17009929, PMID:20144998]
vesiclecellular componentAny small, fluid-filled, spherical organelle enclosed by membrane. [GOC:mah, GOC:pz, GOC:vesicles]
secretory granule lumencellular componentThe volume enclosed by the membrane of a secretory granule. [GOC:rph]
collagen-containing extracellular matrixcellular componentAn extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617]
extracellular exosomecellular componentA vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894]
extracellular vesiclecellular componentAny vesicle that is part of the extracellular region. [GO_REF:0000064, GOC:pm, GOC:TermGenie, PMID:24769233]
ficolin-1-rich granule lumencellular componentAny membrane-enclosed lumen that is part of a ficolin-1-rich granule. [GO_REF:0000064, GOC:TermGenie, PMID:23650620]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Involved In

This protein is involved in 6 target(s):

TargetCategoryDefinition
programmed cell deathbiological processA process which begins when a cell receives an internal or external signal and activates a series of biochemical events (signaling pathway). The process ends with the death of the cell. [GOC:lr, GOC:mtg_apoptosis]
canonical glycolysisbiological processThe glycolytic process that begins with the conversion of glucose to glucose-6-phosphate by glucokinase activity. Glycolytic processes are the chemical reactions and pathways resulting in the breakdown of a carbohydrate into pyruvate, with the concomitant production of a small amount of ATP. [GOC:dph, ISBN:0201090910, ISBN:0879010479]
positive regulation of sprouting angiogenesisbiological processAny process that activates or increases the frequency, rate or extent of sprouting angiogenesis. [GO_REF:0000058, GOC:TermGenie, PMID:16756958]
positive regulation of cytoplasmic translationbiological processAny process that activates or increases the frequency, rate or extent of cytoplasmic translation. [GOC:obol]
glycolytic processbiological processThe chemical reactions and pathways resulting in the breakdown of a carbohydrate into pyruvate, with the concomitant production of a small amount of ATP and the reduction of NAD(P) to NAD(P)H. Glycolysis begins with the metabolism of a carbohydrate to generate products that can enter the pathway and ends with the production of pyruvate. Pyruvate may be converted to acetyl-coenzyme A, ethanol, lactate, or other small molecules. [GOC:bf, GOC:dph, ISBN:0201090910, ISBN:0716720094, ISBN:0879010479, Wikipedia:Glycolysis]
cellular response to insulin stimulusbiological processAny 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 an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732]