Target name

P49840: Glycogen synthase kinase-3 alpha

  Protein function

Constitutively active protein kinase that acts as a negative regulator in the hormonal control of glucose homeostasis, Wnt signaling and regulation of transcription factors and microtubules, by phosphorylating and inactivating glycogen synthase (GYS1 or GYS2), CTNNB1/beta-catenin, APC and AXIN1. Requires primed phosphorylation of the majority of its substrates. Contributes to insulin regulation of glycogen synthesis by phosphorylating and inhibiting GYS1 activity and hence glycogen synthesis. Regulates glycogen metabolism in liver, but not in muscle. May also mediate the development of insulin resistance by regulating activation of transcription factors. In Wnt signaling, regulates the level and transcriptional activity of nuclear CTNNB1/beta-catenin. Facilitates amyloid precursor protein (APP) processing and the generation of APP-derived amyloid plaques found in Alzheimer disease. May be involved in the regulation of replication in pancreatic beta-cells. Is necessary for the establishment of neuronal polarity and axon outgrowth. Through phosphorylation of the anti-apoptotic protein MCL1, may control cell apoptosis in response to growth factors deprivation.

  Database links

Uniprot primary ID P49840
DrugBank ID
BioGrid ID 109186
PharmGKB ID PA29008
KEGG ID hsa:2931
Entrez Gene (Gene ID) 2931
STRING 9606ENSP00000222330
MINT MINT-1688290
IntAct P49840
DMDM 12644292
Rectome R-HSA-5674400 R-HSA-381038 R-HSA-198323
SignaLink P49840
BindingDB P49840

  Model Performance Metrics

Fingerprint type F1_CV AUC_CV Accuracy_CV Sensitivity_CV Specificity_CV F1_test AUC_test Accuracy_test Sensitivity_test Specificity_test Download model
FP2 fingerprints 0.857 0.918 0.866 0.795 0.939 0.878 0.934 0.887 0.831 0.941 Download
MACCS fingerprints 0.811 0.903 0.814 0.791 0.837 0.813 0.913 0.820 0.800 0.838 Download
Daylight fingerprints 0.772 0.834 0.812 0.631 0.996 0.750 0.815 0.805 0.600 1.000 Download
ECFP2 fingerprints 0.868 0.933 0.866 0.869 0.863 0.908 0.941 0.910 0.908 0.912 Download
ECFP4 fingerprints 0.919 0.959 0.919 0.907 0.932 0.915 0.963 0.917 0.908 0.926 Download
ECFP6 fingerprints 0.918 0.955 0.921 0.877 0.966 0.929 0.950 0.932 0.908 0.956 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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