Proteins > Eukaryotic translation initiation factor 2-alpha kinase 1
Page last updated: 2024-08-08 00:12:42

Eukaryotic translation initiation factor 2-alpha kinase 1

A eukaryotic translation initiation factor 2-alpha kinase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9BQI3]

Synonyms

EC 2.7.11.1;
Heme-controlled repressor;
HCR;
Heme-regulated eukaryotic initiation factor eIF-2-alpha kinase;
Heme-regulated inhibitor;
hHRI;
Hemin-sensitive initiation factor 2-alpha kinase

Research

Bioassay Publications (4)

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's4 (100.00)24.3611
2020's0 (0.00)2.80

Compounds (231)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
gsk2656157Homo sapiens (human)IC500.460011
7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1h-indol-5-yl)-7h-pyrrolo(2,3-d)pyrimidin-4-amineHomo sapiens (human)IC500.420011

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
imatinibHomo sapiens (human)Kd20.000022
staurosporineHomo sapiens (human)Kd10.000011
picropodophyllinHomo sapiens (human)Kd30.000011
gefitinibHomo sapiens (human)Kd20.000022
lestaurtinibHomo sapiens (human)Kd20.000022
perifosineHomo sapiens (human)Kd30.000011
vatalanibHomo sapiens (human)Kd23.333323
ruboxistaurinHomo sapiens (human)Kd20.000022
canertinibHomo sapiens (human)Kd20.000022
birb 796Homo sapiens (human)Kd10.000011
cyc 202Homo sapiens (human)Kd30.000011
sb 203580Homo sapiens (human)Kd10.000011
enzastaurinHomo sapiens (human)Kd20.000022
erlotinibHomo sapiens (human)Kd20.000022
lapatinibHomo sapiens (human)Kd20.000022
sorafenibHomo sapiens (human)Kd20.000022
pd 173955Homo sapiens (human)Kd10.000011
s 1033Homo sapiens (human)Kd20.000022
xl147Homo sapiens (human)Kd30.000012
bms 387032Homo sapiens (human)Kd20.000022
sf 2370Homo sapiens (human)Kd30.000011
tandutinibHomo sapiens (human)Kd20.000022
vx-745Homo sapiens (human)Kd10.000011
dasatinibHomo sapiens (human)Kd23.333323
ha 1100Homo sapiens (human)Kd30.000011
7-epi-hydroxystaurosporineHomo sapiens (human)Kd30.000011
zd 6474Homo sapiens (human)Kd20.000022
imd 0354Homo sapiens (human)Kd30.000012
sirolimusHomo sapiens (human)Kd30.000011
alvocidibHomo sapiens (human)Kd0.464022
bosutinibHomo sapiens (human)Kd15.315022
orantinibHomo sapiens (human)Kd30.000011
su 11248Homo sapiens (human)Kd20.000022
palbociclibHomo sapiens (human)Kd30.000011
vx680Homo sapiens (human)Kd20.000022
cyc 116Homo sapiens (human)Kd30.000011
everolimusHomo sapiens (human)Kd30.000011
ekb 569Homo sapiens (human)Kd30.000011
axitinibHomo sapiens (human)Kd20.000022
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)Kd30.000012
y-39983Homo sapiens (human)Kd30.000011
cp 547632Homo sapiens (human)Kd3.572011
bms345541Homo sapiens (human)Kd10.000011
lenvatinibHomo sapiens (human)Kd30.000011
pd 0325901Homo sapiens (human)Kd30.000011
midostaurinHomo sapiens (human)Kd6.023522
px-866Homo sapiens (human)Kd30.000011
ripasudilHomo sapiens (human)Kd30.000011
osi 930Homo sapiens (human)Kd30.000011
ki 20227Homo sapiens (human)Kd10.000011
scio-469Homo sapiens (human)Kd30.000011
cp 724714Homo sapiens (human)Kd30.000011
pi103Homo sapiens (human)Kd10.000011
hmn-214Homo sapiens (human)Kd30.000011
tivozanibHomo sapiens (human)Kd30.000011
hki 272Homo sapiens (human)Kd20.000022
tofacitinibHomo sapiens (human)Kd20.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd3.196022
masitinibHomo sapiens (human)Kd10.000011
ly-2157299Homo sapiens (human)Kd30.000011
pazopanibHomo sapiens (human)Kd20.000022
azd 6244Homo sapiens (human)Kd20.000022
su 14813Homo sapiens (human)Kd20.000022
bibw 2992Homo sapiens (human)Kd20.000022
binimetinibHomo sapiens (human)Kd30.000011
sotrastaurinHomo sapiens (human)Kd30.000012
aee 788Homo sapiens (human)Kd30.000012
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)Kd30.000012
exel-7647Homo sapiens (human)Kd30.000011
volasertibHomo sapiens (human)Kd30.000011
pha 665752Homo sapiens (human)Kd10.000011
azd 7762Homo sapiens (human)Kd30.000011
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)Kd23.333323
brivanibHomo sapiens (human)Kd20.000022
mp470Homo sapiens (human)Kd30.000011
rgb 286638Homo sapiens (human)Kd3.803011
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)Kd10.000011
kw 2449Homo sapiens (human)Kd20.000022
danusertibHomo sapiens (human)Kd30.000011
abt 869Homo sapiens (human)Kd20.000022
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)Kd10.000011
tak 285Homo sapiens (human)Kd30.000011
idelalisibHomo sapiens (human)Kd30.000011
crizotinibHomo sapiens (human)Kd20.000022
osi 906Homo sapiens (human)Kd30.000011
chir-265Homo sapiens (human)Kd20.000022
motesanibHomo sapiens (human)Kd20.000022
fostamatinibHomo sapiens (human)Kd30.000011
trametinibHomo sapiens (human)Kd30.000011
mln8054Homo sapiens (human)Kd20.000022
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)Kd30.000012
dactolisibHomo sapiens (human)Kd30.000011
bgt226Homo sapiens (human)Kd30.000011
gsk 461364Homo sapiens (human)Kd20.000022
azd 1152-hqpaHomo sapiens (human)Kd2.913022
nvp-tae684Homo sapiens (human)Kd10.000011
enmd 2076Homo sapiens (human)Kd30.000011
e 7050Homo sapiens (human)Kd1.080011
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)Kd30.000011
gdc-0973Homo sapiens (human)Kd30.000011
buparlisibHomo sapiens (human)Kd30.000011
azd 1480Homo sapiens (human)Kd30.000011
azd8330Homo sapiens (human)Kd1.821011
pha 848125Homo sapiens (human)Kd30.000011
ro5126766Homo sapiens (human)Kd30.000011
fedratinibHomo sapiens (human)Kd15.500022
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)Kd30.000011
azd5438Homo sapiens (human)Kd30.000011
pf 04217903Homo sapiens (human)Kd30.000011
gdc 0941Homo sapiens (human)Kd23.333323
icotinibHomo sapiens (human)Kd30.000011
ph 797804Homo sapiens (human)Kd30.000012
kx-01Homo sapiens (human)Kd30.000011
plx 4720Homo sapiens (human)Kd10.000011
mk 5108Homo sapiens (human)Kd30.000011
cx 4945Homo sapiens (human)Kd1.661011
cudc 101Homo sapiens (human)Kd30.000011
arry-614Homo sapiens (human)Kd30.000011
tak 593Homo sapiens (human)Kd30.000011
mln 8237Homo sapiens (human)Kd30.000011
sgx 523Homo sapiens (human)Kd20.000022
bms 754807Homo sapiens (human)Kd30.000011
bms 777607Homo sapiens (human)Kd30.000011
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)Kd20.000022
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
dcc-2036Homo sapiens (human)Kd0.666011
cabozantinibHomo sapiens (human)Kd30.000011
defactinibHomo sapiens (human)Kd30.000011
ly2584702Homo sapiens (human)Kd30.000011
incb-018424Homo sapiens (human)Kd20.000022
poziotinibHomo sapiens (human)Kd30.000011
asp3026Homo sapiens (human)Kd30.000011
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)Kd30.000011
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)Kd15.490022
arry-334543Homo sapiens (human)Kd30.000011
kin-193Homo sapiens (human)Kd30.000011
mk 2461Homo sapiens (human)Kd30.000011
bay 869766Homo sapiens (human)Kd30.000011
as 703026Homo sapiens (human)Kd30.000011
baricitinibHomo sapiens (human)Kd0.335011
dabrafenibHomo sapiens (human)Kd0.949011
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)Kd30.000011
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)Kd4.836011
mk-8776Homo sapiens (human)Kd30.000011
afuresertibHomo sapiens (human)Kd30.000011
gsk 1070916Homo sapiens (human)Kd30.000012
jnj38877605Homo sapiens (human)Kd30.000011
dinaciclibHomo sapiens (human)Kd30.000011
gilteritinibHomo sapiens (human)Kd30.000011
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)Kd30.000011
azd1208Homo sapiens (human)Kd30.000011
vx-509Homo sapiens (human)Kd30.000011
debio 1347Homo sapiens (human)Kd30.000011
volitinibHomo sapiens (human)Kd30.000011
osimertinibHomo sapiens (human)Kd30.000011
at 9283Homo sapiens (human)Kd30.000011
otssp167Homo sapiens (human)Kd30.000011
chir 258Homo sapiens (human)Kd20.000022
osi 027Homo sapiens (human)Kd30.000011
nintedanibHomo sapiens (human)Kd20.000022
bay 80-6946Homo sapiens (human)Kd30.000011
pp242Homo sapiens (human)Kd10.000011

Enables

This protein enables 6 target(s):

TargetCategoryDefinition
eukaryotic translation initiation factor 2alpha kinase activitymolecular functionCatalysis of the reaction: ATP + [eukaryotic translation initiation factor 2 alpha subunit] = ADP + [eukaryotic translation initiation factor 2 alpha subunit] phosphate. [GOC:mah, InterPro:IPR015516]
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]
heme bindingmolecular functionBinding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai]
protein homodimerization activitymolecular functionBinding to an identical protein to form a homodimer. [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 1 target(s):

TargetCategoryDefinition
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]

Active In

This protein is active in 3 target(s):

TargetCategoryDefinition
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]
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]

Involved In

This protein is involved in 16 target(s):

TargetCategoryDefinition
acute inflammatory responsebiological processInflammation which comprises a rapid, short-lived, relatively uniform response to acute injury or antigenic challenge and is characterized by accumulations of fluid, plasma proteins, and granulocytic leukocytes. An acute inflammatory response occurs within a matter of minutes or hours, and either resolves within a few days or becomes a chronic inflammatory response. [GO_REF:0000022, GOC:add, ISBN:0781735149]
phagocytosisbiological processA vesicle-mediated transport process that results in the engulfment of external particulate material by phagocytes and their delivery to the lysosome. The particles are initially contained within phagocytic vacuoles (phagosomes), which then fuse with primary lysosomes to effect digestion of the particles. [ISBN:0198506732]
negative regulation of cell population proliferationbiological processAny process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators]
regulation of eIF2 alpha phosphorylation by hemebiological processAny process that modulates the rate, frequency, or extent of eIF2 alpha phosphorylation as a result of heme levels. [GOC:BHF, GOC:dph, GOC:tb]
macrophage differentiationbiological processThe process in which a relatively unspecialized monocyte acquires the specialized features of a macrophage. [GOC:add, ISBN:0781735149]
negative regulation of translational initiation by ironbiological processAny process involving iron that stops, prevents or reduces the rate of translational initiation. [GOC:go_curators]
protoporphyrinogen IX metabolic processbiological processThe chemical reactions and pathways involving protoporphyrinogen IX, the specific substrate for the enzyme ferrochelatase, which catalyzes the insertion of iron to form protoheme. It is probably also the substrate for chlorophyll formation. [ISBN:0198506732]
protein autophosphorylationbiological processThe phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732]
negative regulation of hemoglobin biosynthetic processbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of hemoglobin, an oxygen carrying, conjugated protein containing four heme groups and globin. [GOC:ai]
establishment of localization in cellbiological processAny process, occuring in a cell, that localizes a substance or cellular component. This may occur via movement, tethering or selective degradation. [GOC:ai, GOC:dos, GOC:dph, GOC:tb]
multicellular organismal-level iron ion homeostasisbiological processA chemical homeostatic process involved in the maintenance of a steady state level of iron within extracellular body fluids, such as blood, xylem or phloem, of a multicellular organism. This is distinct from maintenance of cellular homeostasis, which occurs within a cell. [PMID:31431773]
integrated stress response signalingbiological processThe series of molecular signals generated in response to diverse stress stimuli required to restore cellular homeostasis. The core event in this pathway is the phosphorylation of eIF2 alpha by one of four members of the eIF2a kinase family (EIF2AK1/HRI, EIF2AK2/PKR, EIF2AK3/PERK and EIF2AK4/GCN2), which leads to a decrease in global protein synthesis and the induction of selected genes, including the transcription factor ATF4, that together promote cellular recovery. [PMID:27629041]
HRI-mediated signalingbiological processA series of reactions in which a signal is passed on to downstream proteins within the cell via HRI (also known as EIF2AK1), an intracellular protein kinase that is activated by stress signals, such as heme deficiency, oxidative stress, osmotic shock, mitochondrial dysfunction and heat shock. [PMID:27629041]
positive regulation of mitophagybiological processAny process that activates or increases the frequency, rate or extent of mitophagy. [GOC:TermGenie]
response to iron ion starvationbiological 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 starvation stimulus, deprivation of iron ion. [PMID:16208485]
regulation of translational initiation by eIF2 alpha phosphorylationbiological processAny process that modulates the frequency, rate or extent of translation initiation in response to stress by the phosphorylation of eIF2 alpha. [GOC:BHF, GOC:dph, GOC:hjd, GOC:tb]