Target Information
Target General Infomation | |||||
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Target ID |
T44141
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Former ID |
TTDC00247
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Target Name |
Angiopoietin-1
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Gene Name |
ANGPT1
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Synonyms |
ANG-1; ANG1; Angiopoietin1; ANGPT1
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Target Type |
Clinical Trial
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Disease | Breast cancer [ICD9: 174, 175; ICD10: C50] | ||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Function |
Binds and activates TEK/TIE2 receptor by inducing its dimerization and tyrosine phosphorylation. Plays an important role in the regulation of angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Required for normal angiogenesis and heart development during embryogenesis. After birth, activates or inhibits angiogenesis, depending on the context. Inhibits angiogenesis and promotes vascular stability in quiescent vessels, where endothelial cells have tight contacts. In quiescent vessels, ANGPT1 oligomers recruit TEK to cell-cell contacts, forming complexes with TEK molecules from adjoining cells, and this leads to preferential activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascades. In migrating endothelial cells that lack cell-cell adhesions, ANGT1 recruits TEK to contacts with the extracellular matrix, leading to the formation of focal adhesion complexes, activation of PTK2/FAK and of the downstream kinases MAPK1/ERK2 and MAPK3/ERK1, and ultimately to the stimulation of sprouting angiogenesis. Mediates blood vessel maturation/stability. Implicated in endothelial developmental processes laterand distinct from that of VEGF. Appears to play a crucial role in mediating reciprocal interactions between the endothelium and surrounding matrix and mesenchyme.
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BioChemical Class |
Fibrinogen
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Target Validation |
T44141
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UniProt ID | |||||
Sequence |
MTVFLSFAFLAAILTHIGCSNQRRSPENSGRRYNRIQHGQCAYTFILPEHDGNCRESTTD
QYNTNALQRDAPHVEPDFSSQKLQHLEHVMENYTQWLQKLENYIVENMKSEMAQIQQNAV QNHTATMLEIGTSLLSQTAEQTRKLTDVETQVLNQTSRLEIQLLENSLSTYKLEKQLLQQ TNEILKIHEKNSLLEHKILEMEGKHKEELDTLKEEKENLQGLVTRQTYIIQELEKQLNRA TTNNSVLQKQQLELMDTVHNLVNLCTKEGVLLKGGKREEEKPFRDCADVYQAGFNKSGIY TIYINNMPEPKKVFCNMDVNGGGWTVIQHREDGSLDFQRGWKEYKMGFGNPSGEYWLGNE FIFAITSQRQYMLRIELMDWEGNRAYSQYDRFHIGNEKQNYRLYLKGHTGTAGKQSSLIL HGADFSTKDADNDNCMCKCALMLTGGWWFDACGPSNLNGMFYTAGQNHGKLNGIKWHYFK GPSYSLRSTTMMIRPLDF |
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Structure |
4EPU; 4JYO; 4K0V
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Drugs and Mode of Action | |||||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Ras signaling pathway | ||||
Rap1 signaling pathway | |||||
HIF-1 signaling pathway | |||||
PI3K-Akt signaling pathway | |||||
Rheumatoid arthritis | |||||
NetPath Pathway | TGF_beta_Receptor Signaling Pathway | ||||
TNFalpha Signaling Pathway | |||||
FSH Signaling Pathway | |||||
PANTHER Pathway | Angiogenesis | ||||
Pathway Interaction Database | Angiopoietin receptor Tie2-mediated signaling | ||||
SHP2 signaling | |||||
Reactome | Tie2 Signaling | ||||
RAF/MAP kinase cascade | |||||
WikiPathways | Cell surface interactions at the vascular wall | ||||
Angiogenesis | |||||
References | |||||
Ref 523327 | ClinicalTrials.gov (NCT01281254) TRINOVA-2: Trebananib in Ovarian Cancer-2. U.S. National Institutes of Health. |
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