Target name

P42336: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform


  Protein function

Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation in breast cancer cells through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Has also serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS.

  Database links

Uniprot primary ID P42336
PDB ID 4JPS 4WAF 4L1B 4YKN 3ZIM 2RD0 3HIZ 4L23 2ENQ 4TUU 3HHM 4L2Y 4OVU 4TV3 4OVV
DrugBank ID DB00201
BioGrid ID 111308
GuidetoPHARMACOLOGY ID 2153
PharmGKB ID PA33308
KEGG ID hsa:5290
DIP ID DIP-42728N
STRING ID 9606.ENSP00000263967
IntAct ID P42336
DMDM 126302584
BRENDA 2.7.1.137 2.7.1.153
Reactome R-HSA-1660499 R-HSA-4420097 R-HSA-912631 R-HSA-198203 R-HSA-5655332 R-HSA-5654720 R-HSA-114604 R-HSA-389357 R-HSA-2219530 R-HSA-1963642 R-HSA-5654710 R-HSA-5637810 R-HSA-186763 R-HSA-180292 R-HSA-1257604 R-HSA-388841 R-HSA-2029 R-HSA-5654689 R-HSA-2730905
SignaLink P42336
BioCyc MetaCyc:HS04527-MONOMER
Entrez Gene (Gene ID) 5290
BindingDB P42336

  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 0.888 0.004 0.872 0.003 0.880 0.000 0.880 0.000 0.940 0.000 0.760 0.000 Download
Estate fingerprints 0.820 0.000 0.734 0.000 0.777 0.005 0.788 0.004 0.850 0.000 0.552 0.004 Download
MACCS fingerprints 0.851 0.003 0.789 0.000 0.820 0.000 0.830 0.000 0.900 0.000 0.643 0.005 Download
Daylight fingerprints 0.860 0.000 0.772 0.000 0.816 0.005 0.821 0.003 0.870 0.000 0.633 0.005 Download
ECFP2 fingerprints 0.971 0.003 0.893 0.005 0.932 0.004 0.940 0.000 0.990 0.000 0.870 0.000 Download
ECFP4 fingerprints 0.950 0.000 0.970 0.000 0.960 0.000 0.960 0.000 0.990 0.000 0.920 0.000 Download
ECFP6 fingerprints 0.926 0.005 0.990 0.005 0.958 0.004 0.951 0.003 0.990 0.000 0.910 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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