Target name

Q02763: Angiopoietin-1 receptor


  Protein function

Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from blood vessels. Required for normal angiogenesis and heart development during embryogenesis. Required for post-natal hematopoiesis. 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. ANGPT1 signaling triggers receptor dimerization and autophosphorylation at specific tyrosine residues that then serve as binding sites for scaffold proteins and effectors. Signaling is modulated by ANGPT2 that has lower affinity for TEK, can promote TEK autophosphorylation in the absence of ANGPT1, but inhibits ANGPT1-mediated signaling by competing for the same binding site. Signaling is also modulated by formation of heterodimers with TIE1, and by proteolytic processing that gives rise to a soluble TEK extracellular domain. The soluble extracellular domain modulates signaling by functioning as decoy receptor for angiopoietins. TEK phosphorylates DOK2, GRB7, GRB14, PIK3R1; SHC1 and TIE1.

  Database links

Uniprot primary ID Q02763
PDB ID 3L8P 2GY7 2OSC 2WQB 4X3J 1FVR 2OO8 3BEA 4K0V 2GY5 2P4I
DrugBank ID DB05294 DB08896 DB08901 DB00415
BioGrid ID 112869
GuidetoPHARMACOLOGY ID 1842
PharmGKB ID PA36441
KEGG ID hsa:7010
DIP ID DIP-6047N
STRING ID 9606.ENSP00000369375
IntAct ID Q02763
DMDM 218511853
BRENDA 2.7.10.1
Reactome R-HSA-210993 R-HSA-5673001
SignaLink Q02763
BioCyc
Entrez Gene (Gene ID) 7010
BindingDB Q02763

  Model Performance Metrics

Fingerprint type Sensitivity SEN_std Specificity SPE_std Accuracy ACC_std F1-score F1-score_std AUC AUC_std MCC MCC_std Download model
FP2 fingerprints 0.867 0.005 0.913 0.005 0.890 0.000 0.889 0.003 0.950 0.000 0.783 0.007 Download
Estate fingerprints 0.879 0.003 0.763 0.003 0.821 0.003 0.831 0.003 0.893 0.005 0.644 0.007 Download
MACCS fingerprints 0.897 0.005 0.745 0.003 0.821 0.003 0.832 0.004 0.900 0.000 0.648 0.006 Download
Daylight fingerprints 0.791 0.003 0.809 0.005 0.800 0.000 0.799 0.003 0.859 0.003 0.598 0.006 Download
ECFP2 fingerprints 0.930 0.000 0.898 0.005 0.914 0.005 0.916 0.005 0.970 0.000 0.829 0.007 Download
ECFP4 fingerprints 0.880 0.000 0.962 0.005 0.921 0.003 0.919 0.003 0.970 0.000 0.844 0.005 Download
ECFP6 fingerprints 0.834 0.005 0.986 0.005 0.910 0.000 0.904 0.005 0.960 0.000 0.834 0.005 Download

  Download datasets

Positive dataset Negative dataset


Copyright @ 2012-2014 Computational Biology & Drug Design Group,
School of Pharmaceutical Sciences, Central South University. All rights reserved.

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