Target name

P16234: Platelet-derived growth factor receptor alpha


  Protein function

Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for normal skeleton development and cephalic closure during embryonic development. Required for normal development of the mucosa lining the gastrointestinal tract, and for recruitment of mesenchymal cells and normal development of intestinal villi. Plays a role in cell migration and chemotaxis in wound healing. Plays a role in platelet activation, secretion of agonists from platelet granules, and in thrombin-induced platelet aggregation. Binding of its cognate ligands - homodimeric PDGFA, homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFC -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PIK3R1, PLCG1, and PTPN11. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylates PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, and thereby mediates activation of the AKT1 signaling pathway. Mediates activation of HRAS and of the MAP kinases MAPK1/ERK2 and/or MAPK3/ERK1. Promotes activation of STAT family members STAT1, STAT3 and STAT5A and/or STAT5B. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor.

  Database links

Uniprot primary ID P16234
PDB ID 1GQ5
DrugBank ID DB00619 DB00102 DB01268 DB06589 DB08896 DB08901
BioGrid ID 111182
GuidetoPHARMACOLOGY ID 1803
PharmGKB ID PA33147
KEGG ID hsa:5156
DIP ID DIP-5736N
STRING ID 9606.ENSP00000257290
IntAct ID P16234
DMDM 129892
BRENDA 2.7.10.1
Reactome R-HSA-186797 R-HSA-2219530 R-HSA-186763 R-HSA-1257604 R-HSA-5673001
SignaLink P16234
BioCyc
Entrez Gene (Gene ID) 5156
BindingDB P16234

  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 0.857 0.005 0.917 0.005 0.887 0.005 0.881 0.003 0.940 0.000 0.772 0.006 Download
Estate fingerprints 0.765 0.005 0.799 0.006 0.782 0.004 0.780 0.000 0.864 0.005 0.567 0.007 Download
MACCS fingerprints 0.823 0.007 0.811 0.005 0.817 0.005 0.819 0.006 0.880 0.000 0.638 0.008 Download
Daylight fingerprints 0.762 0.004 0.940 0.000 0.851 0.003 0.840 0.000 0.911 0.003 0.716 0.005 Download
ECFP2 fingerprints 0.890 0.007 0.858 0.005 0.874 0.005 0.877 0.005 0.949 0.003 0.748 0.006 Download
ECFP4 fingerprints 0.837 0.005 0.935 0.006 0.886 0.005 0.880 0.000 0.950 0.000 0.775 0.007 Download
ECFP6 fingerprints 0.804 0.005 0.964 0.003 0.884 0.005 0.874 0.005 0.950 0.000 0.777 0.007 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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