Page last updated: 2024-08-07 18:25:44

Serine/threonine-protein kinase PLK4

A serine/threonine-protein kinase PLK4 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00444]

Synonyms

EC 2.7.11.21;
Polo-like kinase 4;
PLK-4;
Serine/threonine-protein kinase 18;
Serine/threonine-protein kinase Sak

Research

Bioassay Publications (16)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (37.50)29.6817
2010's9 (56.25)24.3611
2020's1 (6.25)2.80

Compounds (247)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
go 6976Homo sapiens (human)Ki8.601425
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-oneHomo sapiens (human)Ki13.920015
imatinibHomo sapiens (human)Ki15.050014
staurosporineHomo sapiens (human)IC500.008322
staurosporineHomo sapiens (human)Ki0.535614
sorafenibHomo sapiens (human)Ki17.560014
wortmanninHomo sapiens (human)Ki6.825014
h 1152Homo sapiens (human)Ki15.030014
ellagic acidHomo sapiens (human)IC502.970011
su 11248Homo sapiens (human)Ki12.400014
vx680Homo sapiens (human)Ki8.577247
gw-5074Homo sapiens (human)IC500.230011
axitinibHomo sapiens (human)IC500.045033
axitinibHomo sapiens (human)Ki8.573847
gdp 366Homo sapiens (human)Ki5.101014
cp 547632Homo sapiens (human)Ki15.030014
gw843682xHomo sapiens (human)Ki0.044914
bi 2536Homo sapiens (human)Ki5.000814
Mps1-IN-2Homo sapiens (human)IC503.100010
cfi-400945Homo sapiens (human)IC500.003533
cfi-400945Homo sapiens (human)Ki0.000322
centrinoneHomo sapiens (human)IC500.002922
chir 258Homo sapiens (human)Ki10.562514
r 1530Homo sapiens (human)IC500.007011
r 1530Homo sapiens (human)Ki0.011011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
fasudilHomo sapiens (human)Kd30.000011
4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazolineHomo sapiens (human)Kd30.000011
sb 202190Homo sapiens (human)Kd10.000011
imatinibHomo sapiens (human)Kd13.650044
pyrazolanthroneHomo sapiens (human)Kd0.770011
triciribine phosphateHomo sapiens (human)Kd30.000011
staurosporineHomo sapiens (human)Kd0.000833
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd16.666733
lestaurtinibHomo sapiens (human)Kd0.031033
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd16.666733
ruboxistaurinHomo sapiens (human)Kd9.942544
canertinibHomo sapiens (human)Kd16.666733
birb 796Homo sapiens (human)Kd10.000022
cyc 202Homo sapiens (human)Kd20.000022
sb 203580Homo sapiens (human)Kd10.000022
enzastaurinHomo sapiens (human)Kd20.000022
erlotinibHomo sapiens (human)Kd13.966733
lapatinibHomo sapiens (human)Kd16.666733
sorafenibHomo sapiens (human)Kd9.380055
pd 173955Homo sapiens (human)Kd10.000011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000011
bms 387032Homo sapiens (human)Kd20.000034
sf 2370Homo sapiens (human)Kd0.073011
tandutinibHomo sapiens (human)Kd14.400044
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd16.666733
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd8.185044
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
imd 0354Homo sapiens (human)Kd30.000011
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd12.875044
bosutinibHomo sapiens (human)Kd20.000022
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd5.221766
palbociclibHomo sapiens (human)Kd30.000011
jnj-7706621Homo sapiens (human)Kd0.120011
vx680Homo sapiens (human)Kd0.134844
cyc 116Homo sapiens (human)Kd0.043011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd20.000022
axitinibHomo sapiens (human)Kd0.368522
temsirolimusHomo sapiens (human)Kd30.000011
pd 184352Homo sapiens (human)Kd10.000011
on 01910Homo sapiens (human)Kd30.000011
av 412Homo sapiens (human)Kd30.000011
telatinibHomo sapiens (human)Kd30.000011
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd8.397011
bms345541Homo sapiens (human)Kd10.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd0.102844
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd8.141011
osi 930Homo sapiens (human)Kd30.000011
ki 20227Homo sapiens (human)Kd0.140011
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd20.000022
pi103Homo sapiens (human)Kd10.000022
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd20.000022
tofacitinibHomo sapiens (human)Kd16.666733
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd16.050022
masitinibHomo sapiens (human)Kd20.000022
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd10.193333
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd10.120033
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000011
aee 788Homo sapiens (human)Kd30.000011
saracatinibHomo sapiens (human)Kd30.000011
vx 702Homo sapiens (human)Kd30.000011
crenolanibHomo sapiens (human)Kd30.000011
tg100-115Homo sapiens (human)Kd20.000022
cc 401Homo sapiens (human)Kd30.000011
bms 599626Homo sapiens (human)Kd30.000011
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd0.410011
azd 7762Homo sapiens (human)Kd0.722011
regorafenibHomo sapiens (human)Kd30.000011
6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-oneHomo sapiens (human)Kd0.088622
brivanibHomo sapiens (human)Kd20.000022
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd30.000011
np 031112Homo sapiens (human)Kd30.000011
at 7519Homo sapiens (human)Kd20.000022
bms-690514Homo sapiens (human)Kd30.000011
bi 2536Homo sapiens (human)Kd20.000022
inno-406Homo sapiens (human)Kd30.000011
nvp-ast487Homo sapiens (human)Kd10.000022
kw 2449Homo sapiens (human)Kd0.560522
danusertibHomo sapiens (human)Kd0.005011
abt 869Homo sapiens (human)Kd14.100033
azd 8931Homo sapiens (human)Kd30.000011
arq 197Homo sapiens (human)Kd30.000011
azd 1152Homo sapiens (human)Kd30.000011
pf 00299804Homo sapiens (human)Kd30.000011
ridaforolimusHomo sapiens (human)Kd30.000011
ch 4987655Homo sapiens (human)Kd30.000011
6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamideHomo sapiens (human)Kd30.000011
cc-930Homo sapiens (human)Kd30.000011
gw 2580Homo sapiens (human)Kd10.000022
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd15.030022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd16.666733
motesanibHomo sapiens (human)Kd16.666733
fostamatinibHomo sapiens (human)Kd0.570011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd0.545333
pf-562,271Homo sapiens (human)Kd30.000011
GDC-0879Homo sapiens (human)Kd10.000011
jnj-26483327Homo sapiens (human)Kd30.000011
ly2603618Homo sapiens (human)Kd30.000011
tg100801Homo sapiens (human)Kd30.000011
dactolisibHomo sapiens (human)Kd30.000011
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd20.000022
azd 1152-hqpaHomo sapiens (human)Kd13.133333
nvp-tae684Homo sapiens (human)Kd0.000911
enmd 2076Homo sapiens (human)Kd0.129011
e 7050Homo sapiens (human)Kd30.000011
2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinoneHomo sapiens (human)Kd30.000011
tak-901Homo sapiens (human)Kd0.041011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd0.308011
azd8330Homo sapiens (human)Kd30.000011
pha 848125Homo sapiens (human)Kd30.000011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd1.025022
gsk690693Homo sapiens (human)Kd20.000022
14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaeneHomo sapiens (human)Kd30.000012
azd5438Homo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd16.300022
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000011
kx-01Homo sapiens (human)Kd30.000011
plx 4720Homo sapiens (human)Kd3.500011
mk 5108Homo sapiens (human)Kd0.183011
cx 4945Homo sapiens (human)Kd30.000011
cudc 101Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd30.000011
tak 593Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd1.178011
sgx 523Homo sapiens (human)Kd20.000022
bms 754807Homo sapiens (human)Kd0.010011
bms 777607Homo sapiens (human)Kd0.301011
sgi 1776Homo sapiens (human)Kd30.000011
pci 32765Homo sapiens (human)Kd30.000011
ponatinibHomo sapiens (human)Kd30.000011
amg 900Homo sapiens (human)Kd30.000011
mk-1775Homo sapiens (human)Kd30.000011
AMG-208Homo sapiens (human)Kd30.000011
quizartinibHomo sapiens (human)Kd16.666733
at13148Homo sapiens (human)Kd30.000011
tak 733Homo sapiens (human)Kd30.000011
mk 2206Homo sapiens (human)Kd30.000011
sns 314Homo sapiens (human)Kd30.000011
lucitanibHomo sapiens (human)Kd30.000011
pf-04691502Homo sapiens (human)Kd30.000011
n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamideHomo sapiens (human)Kd0.619011
dcc-2036Homo sapiens (human)Kd4.088011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
ly2584702Homo sapiens (human)Kd30.000012
incb-018424Homo sapiens (human)Kd15.100022
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd0.070011
entrectinibHomo sapiens (human)Kd30.000011
pexidartinibHomo sapiens (human)Kd30.000011
TAK-580Homo sapiens (human)Kd30.000011
gsk 2126458Homo sapiens (human)Kd30.000011
emd1214063Homo sapiens (human)Kd30.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
pf 3758309Homo sapiens (human)Kd0.668011
gdc 0980Homo sapiens (human)Kd30.000011
azd2014Homo sapiens (human)Kd30.000011
(5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanolHomo sapiens (human)Kd30.000011
plx4032Homo sapiens (human)Kd30.000011
gsk 1363089Homo sapiens (human)Kd0.054822
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000012
mk 2461Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000011
baricitinibHomo sapiens (human)Kd30.000012
dabrafenibHomo sapiens (human)Kd0.520011
pki 587Homo sapiens (human)Kd30.000011
n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamideHomo sapiens (human)Kd1.610011
ribociclibHomo sapiens (human)Kd30.000011
mk-8033Homo sapiens (human)Kd30.000011
pha 793887Homo sapiens (human)Kd30.000011
sb 1518Homo sapiens (human)Kd30.000011
abemaciclibHomo sapiens (human)Kd30.000011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
xmd 8-92Homo sapiens (human)Kd0.600010
gsk 1070916Homo sapiens (human)Kd0.575011
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd0.018011
alectinibHomo sapiens (human)Kd30.000011
glpg0634Homo sapiens (human)Kd30.000011
encorafenibHomo sapiens (human)Kd30.000011
bms-911543Homo sapiens (human)Kd30.000011
gsk2141795Homo sapiens (human)Kd30.000011
azd8186Homo sapiens (human)Kd30.000011
byl719Homo sapiens (human)Kd30.000011
cep-32496Homo sapiens (human)Kd30.000011
rociletinibHomo sapiens (human)Kd30.000011
ceritinibHomo sapiens (human)Kd7.100011
azd1208Homo sapiens (human)Kd30.000011
cfi-400945Homo sapiens (human)EC500.012222
vx-509Homo sapiens (human)Kd1.961011
debio 1347Homo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd0.021011
otssp167Homo sapiens (human)Kd0.033011
chir 258Homo sapiens (human)Kd16.666733
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd20.017723
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd0.070011

Enables

This protein enables 5 target(s):

TargetCategoryDefinition
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]
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]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]
protein serine kinase activitymolecular functionCatalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate. [RHEA:17989]

Located In

This protein is located in 8 target(s):

TargetCategoryDefinition
XY bodycellular componentA structure found in a male mammalian spermatocyte containing an unpaired X chromosome that has become densely heterochromatic, silenced and localized at the nuclear periphery. [GOC:hjd, GOC:mr, PMID:20622855, Wikipedia:XY_sex-determination_system]
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]
centrosomecellular componentA structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684]
centriolecellular componentA cellular organelle, found close to the nucleus in many eukaryotic cells, consisting of a small cylinder with microtubular walls, 300-500 nm long and 150-250 nm in diameter. It contains nine short, parallel, peripheral microtubular fibrils, each fibril consisting of one complete microtubule fused to two incomplete microtubules. Cells usually have two centrioles, lying at right angles to each other. At division, each pair of centrioles generates another pair and the twin pairs form the pole of the mitotic spindle. [ISBN:0198547684]
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]
cleavage furrowcellular componentThe cleavage furrow is a plasma membrane invagination at the cell division site. The cleavage furrow begins as a shallow groove and eventually deepens to divide the cytoplasm. [GOC:vw, ISBN:0805319409]
deuterosomecellular componentA spherical, electron dense, cytoplasmic structure that is involved in de novo assembly of centrioles. [GOC:cilia, GOC:dos, PMID:24075808, PMID:25047614, PMID:5661997]
procentriolecellular componentA cellular structure that is the site of a developing centriole, which will become a microtubule organizing center. During the canonical pathway of centriole duplication that occurs during the cell division cycle, procentrioles grow at the proximal ends of both mother and daughter centrioles. In the newly divided cells, the original mother and daughter centrioles become mother centrioles while the procentrioles become the new daughter centrioles. Procentrioles can also arise from de novo pathways that occur in multiciliated cells. In ciliated epithelial cells, numerous procentrioles arise form electron dense material referred to as fibrous granules and deuterosomes. The pathway of procentriole formation in multiciliated protists appears to be similar to that in mammalian multiciliated epithelium. In sperm of primative land plants, multiple procentrioles are formed from a blepharoplast giving rise to multicilated sperm cells. [GOC:bhm, GOC:krc, PMID:18620859, PMID:21289083, PMID

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 1 target(s):

TargetCategoryDefinition
procentriole replication complexcellular componentA protein complex that acts as a chaperone or scaffold for centriolar proteins during the maturation of the procentriole. Some of its members may become integrated into the growing centriole. Examples are the CPAP(CENPJ)-STIL complex, CEP192-PLK4 complex or CEP152-PLK4 complex in vertebrates. [GOC:bhm, PMID:17576815, PMID:18207742, PMID:21059844, PMID:22020124, PMID:24997597]

Involved In

This protein is involved in 6 target(s):

TargetCategoryDefinition
protein phosphorylationbiological processThe process of introducing a phosphate group on to a protein. [GOC:hb]
centriole replicationbiological processThe cell cycle process in which a daughter centriole is formed perpendicular to an existing centriole. An immature centriole contains a ninefold radially symmetric array of single microtubules; mature centrioles consist of a radial array of nine microtubule triplets, doublets, or singlets depending upon the species and cell type. Duplicated centrioles also become the ciliary basal body in cells that form cilia during G0. [GOC:cilia, GOC:kmv, ISBN:0815316194, PMID:9889124]
positive regulation of centriole replicationbiological processAny process that activates or increases the frequency, rate or extent of centriole replication. [GOC:ai]
cilium assemblybiological processThe assembly of a cilium, a specialized eukaryotic organelle that consists of a filiform extrusion of the cell surface. Each cilium is bounded by an extrusion of the cytoplasmic membrane, and contains a regular longitudinal array of microtubules, anchored basally in a centriole. [GOC:BHF, GOC:cilia, GOC:dph, GOC:kmv, GOC:pr, GOC:vw, ISBN:0198506732, PMID:13978319, PMID:27350441, Reactome:R-HSA-5617833.2]
trophoblast giant cell differentiationbiological processThe process in which a relatively unspecialized cell acquires specialized features of a trophoblast giant cell of the placenta. Trophoblast giant cells are the cell of the placenta that line the maternal decidua. [GOC:dph, PMID:16269175]
de novo centriole assembly involved in multi-ciliated epithelial cell differentiationbiological processCentriole assembly in which a centriole arises de novo by a process involving an electron-dense structure known as a deuterosome, rather than by duplication of an existing centriole, and occurring as part of multi-ciliated epithelial cell differentiation. [GOC:cilia, GOC:dos, PMID:24075808, PMID:5111878, PMID:5661997]