Page last updated: 2024-08-07 16:55:22

DNA-dependent protein kinase catalytic subunit

A DNA-dependent protein kinase catalytic subunit that is encoded in the genome of human. [PRO:DNx, UniProtKB:P78527]

Synonyms

DNA-PK catalytic subunit;
DNA-PKcs;
EC 2.7.11.1;
DNPK1;
p460

Research

Bioassay Publications (42)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (30.95)29.6817
2010's27 (64.29)24.3611
2020's2 (4.76)2.80

Compounds (46)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
vanillinHomo sapiens (human)IC501,500.000011
caffeineHomo sapiens (human)IC5010,000.000011
cgs 15943Homo sapiens (human)IC500.140011
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)IC501.32001112
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)Ki6.000033
suraminHomo sapiens (human)IC501.700011
trifluoperazineHomo sapiens (human)IC50100.000011
flavoneHomo sapiens (human)IC5010.000011
alpha-naphthoflavoneHomo sapiens (human)IC504.980011
4,5-dimethoxy-2-nitrobenzaldehydeHomo sapiens (human)IC5015.000011
schizandrin bHomo sapiens (human)IC501,000,000.000011
gefitinibHomo sapiens (human)IC5050.000011
2-(4-morpholinyl)-4h-1-benzopyran-4-oneHomo sapiens (human)IC504.215044
sorafenibHomo sapiens (human)IC5050.000011
wortmanninHomo sapiens (human)Ki0.120022
dasatinibHomo sapiens (human)IC5050.000011
uccf-029Homo sapiens (human)IC5010.000011
ku 55933Homo sapiens (human)IC501.494333
su 11248Homo sapiens (human)IC5050.000011
tanespimycinHomo sapiens (human)IC5040.000011
ic 86621Homo sapiens (human)IC500.120011
nu 7026Homo sapiens (human)IC500.238888
pi103Homo sapiens (human)IC500.021533
nu 7441Homo sapiens (human)IC500.02421212
nu 7441Homo sapiens (human)Ki0.000611
idelalisibHomo sapiens (human)IC506.700022
ku-0060648Homo sapiens (human)IC500.005055
ku 60019Homo sapiens (human)IC500.077011
buparlisibHomo sapiens (human)IC506.917011
ku 0063794Homo sapiens (human)IC5010.000011
gdc 0941Homo sapiens (human)IC501.230011
PP121Homo sapiens (human)IC500.060011
cp 466722Homo sapiens (human)IC500.879011
(3R)-4-[2-(1H-indol-4-yl)-6-(1-methylsulfonylcyclopropyl)-4-pyrimidinyl]-3-methylmorpholineHomo sapiens (human)IC5030.000022
torin 1Homo sapiens (human)IC500.006311
ve 821Homo sapiens (human)IC502.213022
gdc-0032Homo sapiens (human)IC504.800011
torin 2Homo sapiens (human)IC500.000511
cudc-907Homo sapiens (human)IC503.673011
sar245408Homo sapiens (human)IC504.800011
byl719Homo sapiens (human)IC509.100011
cc-115Homo sapiens (human)IC500.014022
vx-970Homo sapiens (human)Ki4.000011
etp-46464Homo sapiens (human)IC500.036011
isogranulatimideHomo sapiens (human)IC5010.000011
pp242Homo sapiens (human)IC501.8292315

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
nu 7441Homo sapiens (human)EC500.212011
ku-0060648Homo sapiens (human)EC500.136011
buparlisibHomo sapiens (human)Kd1.800011
gdc 0941Homo sapiens (human)Kd1.300011
gdc 0980Homo sapiens (human)Kd9.800011
pki 587Homo sapiens (human)Kd30.000011
torin 2Homo sapiens (human)EC500.118011

Enables

This protein enables 13 target(s):

TargetCategoryDefinition
double-stranded DNA bindingmolecular functionBinding to double-stranded DNA. [GOC:elh, GOC:vw]
RNA bindingmolecular functionBinding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah]
protein kinase activitymolecular functionCatalysis 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 activitymolecular functionCatalysis 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]
DNA-dependent protein kinase activitymolecular functionDNA dependent catalysis of the reaction: ATP + a protein = ADP + a phosphoprotein. [GOC:mah]
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]
enzyme bindingmolecular functionBinding to an enzyme, a protein with catalytic activity. [GOC:jl]
protein domain specific bindingmolecular functionBinding to a specific domain of a protein. [GOC:go_curators]
U3 snoRNA bindingmolecular functionBinding to a U3 small nucleolar RNA. [GOC:mah]
histone H2AXS139 kinase activitymolecular functionCatalysis of the reaction: histone H2AX-serine (position 139) + ATP = histone H2AX-phosphoserine (position 139) + ADP. This reaction is the addition of a phosphate group to the serine residue at position 139 of histone variant H2AX. [GOC:yaf, PMID:11893489, PMID:16061642]
RNA polymerase II-specific DNA-binding transcription factor bindingmolecular functionBinding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 6 target(s):

TargetCategoryDefinition
chromosome, telomeric regioncellular componentThe end of a linear chromosome, required for the integrity and maintenance of the end. A chromosome telomere usually includes a region of telomerase-encoded repeats the length of which rarely exceeds 20 bp each and that permits the formation of a telomeric loop (T-loop). The telomeric repeat region is usually preceded by a sub-telomeric region that is gene-poor but rich in repetitive elements. Some telomeres only consist of the latter part (for eg. D. melanogaster telomeres). [GOC:elh]
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]
nucleoplasmcellular componentThat part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
nucleoluscellular componentA 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]
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]
membranecellular componentA lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
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]

Part Of

This protein is part of 8 target(s):

TargetCategoryDefinition
DNA-dependent protein kinase complexcellular componentA protein complex that is involved in the repair of DNA double-strand breaks and, in mammals, V(D)J recombination events. It consists of the DNA-dependent protein kinase catalytic subunit (DNA-PKcs) and the DNA end-binding heterodimer Ku. [GOC:mah, PMID:10854421, PMID:12235392]
chromatincellular componentThe ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130]
transcription regulator complexcellular componentA protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl]
DNA-dependent protein kinase-DNA ligase 4 complexcellular componentA large protein complex which is involved in the repair of DNA double-strand breaks and, in mammals, V(D)J recombination events. It consists of the DNA-dependent protein kinase catalytic subunit (DNA-PKcs), the DNA end-binding heterodimer Ku, the nuclear phosphoprotein XRCC4 or a homolog thereof, and DNA ligase IV. [GOC:jl, GOC:mah, PMID:10854421, PMID:12235392, PMID:17072889]
small-subunit processomecellular componentA large ribonucleoprotein complex that is an early preribosomal complex. In S. cerevisiae, it has a size of 80S and consists of the 35S pre-rRNA, early-associating ribosomal proteins most of which are part of the small ribosomal subunit, the U3 snoRNA and associated proteins. [GOC:krc, GOC:vw, PMID:12068309, PMID:12957375, PMID:15120992, PMID:15590835]
protein-containing complexcellular componentA stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah]
protein-DNA complexcellular componentA macromolecular complex containing both protein and DNA molecules. [GOC:mah]
nonhomologous end joining complexcellular componentA protein complex that plays a role in DNA double-strand break repair via nonhomologous end joining. Such complexes typically contain a specialized DNA ligase (e.g. Lig4 in eukaryotes) and one or more proteins that bind to DNA ends. [GOC:mah, PMID:17072889, PMID:17938628]

Involved In

This protein is involved in 46 target(s):

TargetCategoryDefinition
maturation of 5.8S rRNAbiological processAny process involved in the maturation of a precursor 5.8S ribosomal RNA (rRNA) molecule into a mature 5.8S rRNA molecule. [GOC:curators]
somitogenesisbiological processThe formation of mesodermal clusters that are arranged segmentally along the anterior posterior axis of an embryo. [ISBN:0721662544]
negative regulation of protein phosphorylationbiological processAny process that stops, prevents or reduces the rate of addition of phosphate groups to amino acids within a protein. [GOC:hjd]
activation of innate immune responsebiological processAny process that initiates an innate immune response. Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. Examples of this process include activation of the hypersensitive response of Arabidopsis thaliana and activation of any NOD or TLR signaling pathway in vertebrate species. [GO_REF:0000022, GOC:add, GOC:mtg_sensu, ISBN:0781735149, PMID:15199967, PMID:16177805]
B cell lineage commitmentbiological processThe process in which a lymphoid progenitor cell becomes committed to become any type of B cell. [GOC:add, ISBN:0781735149]
immature B cell differentiationbiological processThe process in which a precursor cell type acquires the specialized features of an immature B cell. [GOC:jal, ISBN:0781735149, PMID:16551251]
pro-B cell differentiationbiological processThe process in which a precursor cell type acquires the specialized features of a pro-B cell. Pro-B cells are the earliest stage of the B cell lineage and undergo heavy chain D and J gene rearrangements, although they are not fully committed. [GOC:jal, ISBN:0781735149]
T cell lineage commitmentbiological processThe process in which a lymphoid progenitor cell becomes committed to becoming any type of T cell. [GOC:add, ISBN:0781735149]
double-strand break repairbiological processThe repair of double-strand breaks in DNA via homologous and nonhomologous mechanisms to reform a continuous DNA helix. [GOC:elh]
double-strand break repair via nonhomologous end joiningbiological processThe repair of a double-strand break in DNA in which the two broken ends are rejoined with little or no sequence complementarity. Information at the DNA ends may be lost due to the modification of broken DNA ends. This term covers instances of separate pathways, called classical (or canonical) and alternative nonhomologous end joining (C-NHEJ and A-NHEJ). These in turn may further branch into sub-pathways, but evidence is still unclear. [GOC:rph, PMID:10827453, PMID:24837021]
chromatin remodelingbiological processA dynamic process of chromatin reorganization resulting in changes to chromatin structure. These changes allow DNA metabolic processes such as transcriptional regulation, DNA recombination, DNA repair, and DNA replication. [GOC:jid, GOC:vw, PMID:12042764, PMID:12697820]
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
DNA damage responsebiological 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 a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators]
brain developmentbiological processThe process whose specific outcome is the progression of the brain over time, from its formation to the mature structure. Brain development begins with patterning events in the neural tube and ends with the mature structure that is the center of thought and emotion. The brain is responsible for the coordination and control of bodily activities and the interpretation of information from the senses (sight, hearing, smell, etc.). [GOC:dph, GOC:jid, GOC:tb, UBERON:0000955]
heart developmentbiological processThe process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948]
response to gamma radiationbiological processAny 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 gamma radiation stimulus. Gamma radiation is a form of electromagnetic radiation (EMR) or light emission of a specific frequency produced from sub-atomic particle interaction, such as electron-positron annihilation and radioactive decay. Gamma rays are generally characterized as EMR having the highest frequency and energy, and also the shortest wavelength, within the electromagnetic radiation spectrum. [GOC:tair_curators]
telomere cappingbiological processA process in which telomeres are protected from degradation and fusion, thereby ensuring chromosome stability by protecting the ends from both degradation and from being recognized as damaged DNA. May be mediated by specific single- or double-stranded telomeric DNA binding proteins. [GOC:mah, GOC:rn, PMID:11349150, PMID:11352055]
peptidyl-serine phosphorylationbiological processThe phosphorylation of peptidyl-serine to form peptidyl-O-phospho-L-serine. [RESID:AA0037]
peptidyl-threonine phosphorylationbiological processThe phosphorylation of peptidyl-threonine to form peptidyl-O-phospho-L-threonine. [RESID:AA0038]
mitotic G1 DNA damage checkpoint signalingbiological processA signal transduction process that contributes to a mitotic cell cycle G1/S transition DNA damage checkpoint. [GOC:mtg_cell_cycle]
protein destabilizationbiological processAny process that decreases the stability of a protein, making it more vulnerable to degradative processes or aggregation. [GOC:mah]
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]
T cell differentiation in thymusbiological processThe process in which a precursor cell type acquires the specialized features of a T cell via a differentiation pathway dependent upon transit through the thymus. [GOC:add, ISBN:0781735149]
T cell receptor V(D)J recombinationbiological processThe process in which T cell receptor V, D, and J, or V and J gene segments, depending on the specific locus, are recombined within a single locus utilizing the conserved heptamer and nonomer recombination signal sequences (RSS). [GOC:add, ISBN:0781700221]
small-subunit processome assemblybiological processThe aggregation, arrangement and bonding together of proteins and RNA molecules to form a small-subunit processome. [GOC:mah]
ectopic germ cell programmed cell deathbiological processProgrammed cell death of an errant germ line cell that is outside the normal migratory path or ectopic to the gonad. This is an important mechanism of regulating germ cell survival within the embryo. [PMID:12814944]
protein modification processbiological processThe covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl]
regulation of circadian rhythmbiological processAny process that modulates the frequency, rate or extent of a circadian rhythm. A circadian rhythm is a biological process in an organism that recurs with a regularity of approximately 24 hours. [GOC:dph, GOC:jl, GOC:tb]
positive regulation of apoptotic processbiological processAny process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
negative regulation of apoptotic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
innate immune responsebiological processInnate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu]
positive regulation of lymphocyte differentiationbiological processAny process that activates or increases the frequency, rate or extent of lymphocyte differentiation. [GOC:go_curators]
positive regulation of erythrocyte differentiationbiological processAny process that activates or increases the frequency, rate or extent of erythrocyte differentiation. [GOC:go_curators]
positive regulation of translationbiological processAny process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of proteins by the translation of mRNA or circRNA. [GOC:dph, GOC:go_curators, GOC:tb]
positive regulation of transcription by RNA polymerase IIbiological processAny process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH]
rhythmic processbiological processAny process pertinent to the generation and maintenance of rhythms in the physiology of an organism. [GOC:jid]
regulation of smooth muscle cell proliferationbiological processAny process that modulates the frequency, rate or extent of smooth muscle cell proliferation. [CL:0000192, GOC:ebc]
regulation of epithelial cell proliferationbiological processAny process that modulates the frequency, rate or extent of epithelial cell proliferation. [GOC:ai]
double-strand break repair via alternative nonhomologous end joiningbiological processAn instance of double-strand break repair via nonhomologous end joining that is independent of factors important for V(D)J recombination (as opposed to classical nonhomologous end joining). It often results in a deletion with microhomology (i.e. 5-25bp homology) at the repair junction. Among different subclasses of nonhomologous end joining (NHEJ), alternative NHEJ appears to play a significant role in the etiology of mutations that arise during cancer development and treatment. [GOC:rph, PMID:18584027, PMID:21655080, Wikipedia:Microhomology-mediated_end_joining]
negative regulation of cGAS/STING signaling pathwaybiological processAny process that stops, prevents or reduces the frequency, rate or extent of cGAS/STING signaling pathway. [PMID:29875158]
regulation of hematopoietic stem cell differentiationbiological processAny process that modulates the frequency, rate or extent of hematopoietic stem cell differentiation. [GOC:TermGenie, PMID:23403623]
positive regulation of platelet formationbiological processAny process that activates or increases the frequency, rate or extent of platelet formation. [GO_REF:0000058, GOC:TermGenie, PMID:10606160]
positive regulation of double-strand break repair via nonhomologous end joiningbiological processAny process that activates or increases the frequency, rate or extent of double-strand break repair via nonhomologous end joining. [GOC:obol]
immunoglobulin V(D)J recombinationbiological processThe process in which immunoglobulin gene segments are recombined within a single locus utilizing the conserved heptamer and nonomer recombination signal sequences (RSS). For immunoglobulin heavy chains V, D, and J gene segments are joined, and for immunoglobulin light chains V and J gene segments are joined. [GOC:add, ISBN:0781735149]
telomere maintenancebiological processAny process that contributes to the maintenance of proper telomeric length and structure by affecting and monitoring the activity of telomeric proteins, the length of telomeric DNA and the replication and repair of the DNA. These processes includes those that shorten, lengthen, replicate and repair the telomeric DNA sequences. [GOC:BHF, GOC:BHF_telomere, GOC:elh, GOC:rl, PMID:11092831]
intrinsic apoptotic signaling pathway in response to DNA damagebiological processThe 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 detection of DNA damage, and ends when the execution phase of apoptosis is triggered. [GOC:go_curators, GOC:mtg_apoptosis]