Target name

P17948: Vascular endothelial growth factor receptor 1


  Protein function

Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. Can promote endothelial cell proliferation, survival and angiogenesis in adulthood. Its function in promoting cell proliferation seems to be cell-type specific. Promotes PGF-mediated proliferation of endothelial cells, proliferation of some types of cancer cells, but does not promote proliferation of normal fibroblasts (in vitro). Has very high affinity for VEGFA and relatively low protein kinase activity; may function as a negative regulator of VEGFA signaling by limiting the amount of free VEGFA and preventing its binding to KDR. Likewise, isoforms lacking a transmembrane domain, such as isoform 2, isoform 3 and isoform 4, may function as decoy receptors for VEGFA. Modulates KDR signaling by forming heterodimers with KDR. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leading to activation of phosphatidylinositol kinase and the downstream signaling pathway. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Phosphorylates SRC and YES1, and may also phosphorylate CBL. Isoform 1 phosphorylates PLCG. Promotes phosphorylation of AKT1 at 'Ser-473'. Promotes phosphorylation of PTK2/FAK1. Isoform 7 has a truncated kinase domain; it increases phosphorylation of SRC at 'Tyr-418' by unknown means and promotes tumor cell invasion.

  Database links

Uniprot primary ID P17948
PDB ID 4CL7 1QSZ 2XAC 1FLT 1QTY 1QSV 1RV6 4CKV 3HNG
DrugBank ID DB09079 DB09078 DB06626 DB01268 DB06589 DB08896 DB00398
BioGrid ID 108609
GuidetoPHARMACOLOGY ID 1812
PharmGKB ID PA28180
KEGG ID hsa:2321
DIP ID DIP-643N
STRING ID 9606.ENSP00000282397
IntAct ID P17948
DMDM 143811474
BRENDA 2.7.10.1
Reactome R-HSA-195399 R-HSA-194306
SignaLink P17948
BioCyc
Entrez Gene (Gene ID) 2321
BindingDB P17948

  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 0.879 0.003 0.881 0.005 0.880 0.000 0.880 0.000 0.950 0.000 0.761 0.003 Download
Estate fingerprints 0.846 0.005 0.748 0.005 0.797 0.005 0.807 0.005 0.890 0.000 0.596 0.005 Download
MACCS fingerprints 0.836 0.005 0.738 0.007 0.787 0.005 0.797 0.005 0.880 0.000 0.574 0.005 Download
Daylight fingerprints 0.905 0.007 0.811 0.005 0.858 0.004 0.863 0.005 0.919 0.003 0.714 0.010 Download
ECFP2 fingerprints 0.893 0.005 0.879 0.005 0.886 0.005 0.889 0.003 0.954 0.005 0.772 0.006 Download
ECFP4 fingerprints 0.875 0.005 0.939 0.005 0.907 0.005 0.903 0.005 0.960 0.000 0.815 0.005 Download
ECFP6 fingerprints 0.840 0.000 0.980 0.000 0.910 0.000 0.900 0.000 0.960 0.000 0.820 0.000 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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