Page last updated: 2024-08-07 16:59:43

Angiopoietin-1 receptor

An angiopoietin-1 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q02763]

Synonyms

EC 2.7.10.1;
Endothelial tyrosine kinase;
Tunica interna endothelial cell kinase;
Tyrosine kinase with Ig and EGF homology domains-2;
Tyrosine-protein kinase receptor TEK;
Tyrosine-protein kinase receptor TIE-2;
hTIE2;
p140 TE

Research

Bioassay Publications (60)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's27 (45.00)29.6817
2010's31 (51.67)24.3611
2020's2 (3.33)2.80

Compounds (104)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
niclosamideHomo sapiens (human)IC5067.800011
staurosporineHomo sapiens (human)IC509,916.735266
ptk 787Homo sapiens (human)IC5010.000011
birb 796Homo sapiens (human)IC503.675033
sb 203580Homo sapiens (human)IC5020.000011
sorafenibHomo sapiens (human)IC500.003255
N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-1-naphthalenecarboxamideHomo sapiens (human)IC5010.000011
zd 6474Homo sapiens (human)IC501.533522
sulfuretinHomo sapiens (human)IC500.950011
ellagic acidHomo sapiens (human)IC500.260011
bosutinibHomo sapiens (human)IC501.191011
semaxinibHomo sapiens (human)IC5010.000011
su 11248Homo sapiens (human)IC500.018011
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-oneHomo sapiens (human)IC5024.000011
2-((4-pyridyl)methyl)amino-n-(3-(trifluoromethyl)phenyl)benzamideHomo sapiens (human)IC5010.000011
a 419259Homo sapiens (human)IC501.012158
gdp 366Homo sapiens (human)IC500.454658
b 43Homo sapiens (human)IC504.343333
a 770041Homo sapiens (human)IC5050.000011
cp 547632Homo sapiens (human)IC500.319022
chir 99021Homo sapiens (human)IC505.000011
regorafenibHomo sapiens (human)IC500.156222
abt 869Homo sapiens (human)IC500.060127
gw 2580Homo sapiens (human)IC5020.000011
tak 285Homo sapiens (human)IC5010.000011
crizotinibHomo sapiens (human)IC500.226522
N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]carbamic acid (2,6-dimethylphenyl) esterHomo sapiens (human)IC500.487014
nvp-tae684Homo sapiens (human)IC504.393033
cefpodoximeHomo sapiens (human)IC5010.125022
amg 458Homo sapiens (human)IC501.000011
bms 777607Homo sapiens (human)IC500.500011
cabozantinibHomo sapiens (human)IC500.014355
gsk 1363089Homo sapiens (human)IC500.001111
tak-632Homo sapiens (human)IC500.740011
gsk 1070916Homo sapiens (human)IC500.059021
chir 98014Homo sapiens (human)IC505.000011
dcc-2701Homo sapiens (human)IC500.008022
cfi-400945Homo sapiens (human)IC500.022011

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
cetirizineHomo sapiens (human)Kd90.000011
loperamideHomo sapiens (human)Kd5.900011
sb 202190Homo sapiens (human)Kd10.000011
imatinibHomo sapiens (human)Kd10.000022
ampicillinHomo sapiens (human)Kd82.000011
staurosporineHomo sapiens (human)Kd0.173333
gefitinibHomo sapiens (human)Kd10.000022
lestaurtinibHomo sapiens (human)Kd0.630022
vatalanibHomo sapiens (human)Kd10.000022
ruboxistaurinHomo sapiens (human)Kd10.000022
canertinibHomo sapiens (human)Kd10.000022
birb 796Homo sapiens (human)Kd0.017033
cyc 202Homo sapiens (human)Kd10.000011
sb 203580Homo sapiens (human)Kd10.000022
enzastaurinHomo sapiens (human)Kd10.000011
erlotinibHomo sapiens (human)Kd10.000022
lapatinibHomo sapiens (human)Kd10.000022
sorafenibHomo sapiens (human)Kd2.325044
pd 173955Homo sapiens (human)Kd0.280011
s 1033Homo sapiens (human)Kd1.000011
bms 387032Homo sapiens (human)Kd10.000022
tandutinibHomo sapiens (human)Kd10.000033
vx-745Homo sapiens (human)Kd10.000022
dasatinibHomo sapiens (human)Kd10.000022
zd 6474Homo sapiens (human)Kd1.866733
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1h-imidazol-2-yl)benzamideHomo sapiens (human)Kd10.000011
alvocidibHomo sapiens (human)Kd10.000022
bosutinibHomo sapiens (human)Kd3.900011
su 11248Homo sapiens (human)Kd10.000033
jnj-7706621Homo sapiens (human)Kd0.950011
vx680Homo sapiens (human)Kd0.450022
ekb 569Homo sapiens (human)Kd6.450022
axitinibHomo sapiens (human)Kd0.310011
pd 184352Homo sapiens (human)Kd10.000011
bms345541Homo sapiens (human)Kd10.000011
midostaurinHomo sapiens (human)Kd1.900033
ki 20227Homo sapiens (human)Kd10.000011
cp 724714Homo sapiens (human)Kd10.000011
pi103Homo sapiens (human)Kd10.000022
hki 272Homo sapiens (human)Kd3.000011
tofacitinibHomo sapiens (human)Kd10.000022
n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamideHomo sapiens (human)Kd10.000011
cediranibHomo sapiens (human)Kd0.140011
masitinibHomo sapiens (human)Kd10.000011
pazopanibHomo sapiens (human)Kd6.650022
azd 6244Homo sapiens (human)Kd10.000011
su 14813Homo sapiens (human)Kd10.000022
bibw 2992Homo sapiens (human)Kd10.000011
tg100-115Homo sapiens (human)Kd10.000011
pha 665752Homo sapiens (human)Kd6.700011
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)Kd0.310011
brivanibHomo sapiens (human)Kd0.440011
at 7519Homo sapiens (human)Kd10.000011
bi 2536Homo sapiens (human)Kd10.000011
nvp-ast487Homo sapiens (human)Kd0.019022
kw 2449Homo sapiens (human)Kd1.100011
abt 869Homo sapiens (human)Kd0.450022
gw 2580Homo sapiens (human)Kd10.000022
crizotinibHomo sapiens (human)Kd0.270011
chir-265Homo sapiens (human)Kd1.300022
motesanibHomo sapiens (human)Kd10.000022
mln8054Homo sapiens (human)Kd0.300022
GDC-0879Homo sapiens (human)Kd10.000011
gsk 461364Homo sapiens (human)Kd10.000011
azd 1152-hqpaHomo sapiens (human)Kd1.900022
nvp-tae684Homo sapiens (human)EC501.167011
nvp-tae684Homo sapiens (human)Kd0.046011
fedratinibHomo sapiens (human)Kd1.900011
gsk690693Homo sapiens (human)Kd10.000011
gdc 0941Homo sapiens (human)Kd10.000011
plx 4720Homo sapiens (human)Kd10.000011
sgx 523Homo sapiens (human)Kd10.000011
quizartinibHomo sapiens (human)Kd10.000022
incb-018424Homo sapiens (human)Kd10.000011
gsk 1838705aHomo sapiens (human)Kd10.000011
gsk 1363089Homo sapiens (human)Kd0.003111
cfi-400945Homo sapiens (human)EC500.117022
chir 258Homo sapiens (human)Kd10.000022
nintedanibHomo sapiens (human)Kd1.400011
pp242Homo sapiens (human)Kd2.200011

Enables

This protein enables 7 target(s):

TargetCategoryDefinition
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]
transmembrane receptor protein tyrosine kinase activitymolecular functionCombining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, 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]
growth factor bindingmolecular functionBinding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators]
signaling receptor activitymolecular functionReceiving a signal and transmitting it in the cell to initiate a change in cell activity. A signal is a physical entity or change in state that is used to transfer information in order to trigger a response. [GOC:bf, GOC:signaling]
identical protein bindingmolecular functionBinding to an identical protein or proteins. [GOC:jl]

Located In

This protein is located in 12 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]
cytoplasmcellular componentThe contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
microvilluscellular componentThin cylindrical membrane-covered projections on the surface of an animal cell containing a core bundle of actin filaments. Present in especially large numbers on the absorptive surface of intestinal cells. [ISBN:0815316194]
cell-cell junctioncellular componentA cell junction that forms a connection between two or more cells of an organism; excludes direct cytoplasmic intercellular bridges, such as ring canals in insects. [GOC:aruk, GOC:bc, GOC:dgh, GOC:hb, GOC:mah, PMID:21422226, PMID:28096264]
focal adhesioncellular componentA cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002]
basal plasma membranecellular componentThe region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators]
cell surfacecellular componentThe external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm]
basolateral plasma membranecellular componentThe region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators]
apical plasma membranecellular componentThe region of the plasma membrane located at the apical end of the cell. [GOC:curators]
centriolar satellitecellular componentA small (70-100 nm) cytoplasmic granule that contains a number of centrosomal proteins; centriolar satellites traffic toward microtubule minus ends and are enriched near the centrosome. [GOC:BHF, PMID:10579718, PMID:12403812]
membrane raftcellular componentAny of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Part Of

This protein is part of 1 target(s):

TargetCategoryDefinition
receptor complexcellular componentAny protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators]

Involved In

This protein is involved in 36 target(s):

TargetCategoryDefinition
angiogenesisbiological processBlood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453]
response to hypoxiabiological 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 stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd]
positive regulation of protein phosphorylationbiological processAny process that activates or increases the frequency, rate or extent of addition of phosphate groups to amino acids within a protein. [GOC:hjd]
endothelial cell proliferationbiological processThe multiplication or reproduction of endothelial cells, resulting in the expansion of a cell population. Endothelial cells are thin flattened cells which line the inside surfaces of body cavities, blood vessels, and lymph vessels, making up the endothelium. [GOC:add, ISBN:0781735149]
positive regulation of endothelial cell proliferationbiological processAny process that activates or increases the rate or extent of endothelial cell proliferation. [GOC:add]
endochondral ossificationbiological processReplacement ossification wherein bone tissue replaces cartilage. [GO_REF:0000034, ISBN:0878932437]
sprouting angiogenesisbiological processThe extension of new blood vessels from existing vessels into avascular tissues, this process includes the specialization of endothelial cells into leading tip and stalk cells, proliferation and migration of the endothelial cells and cell adhesion resulting in angiogenic sprout fusion or lumen formation. [PMID:16391003, PMID:23031691]
cell surface receptor protein tyrosine kinase signaling pathwaybiological processThe series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling]
cell-cell signalingbiological processAny process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah]
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]
positive regulation of endothelial cell migrationbiological processAny process that increases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb]
negative regulation of angiogenesisbiological processAny process that stops, prevents, or reduces the frequency, rate or extent of angiogenesis. [GOC:go_curators]
regulation of establishment or maintenance of cell polaritybiological processAny process that modulates the frequency, rate or extent of the specification, formation or maintenance of anisotropic intracellular organization or cell growth patterns. [GOC:mah]
substrate adhesion-dependent cell spreadingbiological processThe morphogenetic process that results in flattening of a cell as a consequence of its adhesion to a substrate. [GOC:mah, GOC:pf, PMID:17050732]
positive regulation of Rac protein signal transductionbiological processAny process that activates or increases the frequency, rate or extent of Rac protein signal transduction. [GOC:bf]
positive regulation of Rho protein signal transductionbiological processAny process that activates or increases the frequency, rate or extent of Rho protein signal transduction. [GOC:bf]
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]
regulation of vascular permeabilitybiological processAny process that modulates the extent to which blood vessels can be pervaded by fluid. [GOC:jl]
response to peptide hormonebiological 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 peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [PMID:11027914, PMID:15134857, Wikipedia:Peptide_hormone]
response to estrogenbiological 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 stimulus by an estrogen, C18 steroid hormones that can stimulate the development of female sexual characteristics. [GOC:jl, ISBN:0198506732]
positive regulation of angiogenesisbiological processAny process that activates or increases angiogenesis. [GOC:go_curators]
Tie signaling pathwaybiological processThe series of molecular signals initiated by an angiopoietin binding to the Tie receptor, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling, PMID:11283723, PMID:11566266]
negative regulation of inflammatory responsebiological processAny process that stops, prevents, or reduces the frequency, rate or extent of the inflammatory response. [GOC:ai]
response to cAMPbiological 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 cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate) stimulus. [GOC:ai]
positive regulation of focal adhesion assemblybiological processAny process that activates or increases the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai]
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionbiological processAny process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai]
definitive hemopoiesisbiological processA second wave of blood cell production that, in vertebrates, generates long-term hemopoietic stem cells that continously provide erythroid, myeloid and lymphoid lineages throughout adulthood. [GOC:bf, GOC:dph, PMID:15378083, PMID:15617691]
heart trabecula formationbiological processThe process of creating a trabecula in the heart. A trabecula is a tissue element in the form of a small beam, strut or rod. [GOC:dph]
positive regulation of ERK1 and ERK2 cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
glomerulus vasculature developmentbiological processThe biological process whose specific outcome is the progression of a glomerulus vasculature from an initial condition to its mature state. This process begins with the formation of the glomerulus vasculature and ends with the mature structure. The glomerulus vasculature is composed of the tubule structures that carry blood or lymph in the glomerulus. [GOC:mtg_kidney_jan10]
positive regulation of intracellular signal transductionbiological processAny process that activates or increases the frequency, rate or extent of intracellular signal transduction. [GOC:BHF, GOC:dph, GOC:signaling, GOC:tb, GOC:TermGenie]
regulation of endothelial cell apoptotic processbiological processAny process that modulates the frequency, rate or extent of endothelial cell apoptotic process. [GOC:mah, GOC:mtg_apoptosis]
negative regulation of endothelial cell apoptotic processbiological processAny process that stops, prevents or reduces the frequency, rate or extent of endothelial cell apoptotic process. [GOC:BHF, GOC:mah, GOC:mtg_apoptosis]
positive regulation of MAPK cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators]
positive regulation of kinase activitybiological processAny process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah]
multicellular organism developmentbiological processThe biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb]