TargetNet


Q07912

Activated CDC42 kinase 1


Function

Non-receptor tyrosine-protein and serine/threonine- protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals to cytosolic and nuclear effectors. Phosphorylates AKT1, AR, MCF2, WASL and WWOX. Implicated in trafficking and clathrin-mediated endocytosis through binding to epidermal growth factor receptor (EGFR) and clathrin. Binds to both poly- and mono-ubiquitin and regulates ligand-induced degradation of EGFR, thereby contributing to the accumulation of EGFR at the limiting membrane of early endosomes. Downstream effector of CDC42 which mediates CDC42-dependent cell migration via phosphorylation of BCAR1. May be involved both in adult synaptic function and plasticity and in brain development. Activates AKT1 by phosphorylating it on 'Tyr-176'. Phosphorylates AR on 'Tyr-267' and 'Tyr-363' thereby promoting its recruitment to androgen-responsive enhancers (AREs). Phosphorylates WWOX on 'Tyr- 287'. Phosphorylates MCF2, thereby enhancing its activity as a guanine nucleotide exchange factor (GEF) toward Rho family proteins. Contributes to the control of AXL receptor levels. Confers metastatic properties on cancer cells and promotes tumor growth by negatively regulating tumor suppressor such as WWOX and positively regulating pro-survival factors such as AKT1 and AR.


Database Links

Database Links
UniProt Q07912
PDB 1CF4, 1U46, 1U4D, 1U54, 3EQP, 3EQR, 4EWH, 4HZR, 4HZS, 4ID7
BioGrid 115485
BindingDB Q07912
DrugBank DB00171
Guide to PHARMACOLOGY 2246
PharmGKB PA134909759
KEGG hsa:10188
BioCyc Not available
Entrez Gene (GeneID) 10188

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9625 0.0038
Accuracy 0.9216 0.0056
Sensitivity 0.9285 0.0091
Specificity 0.914 0.0049
BEDROC 0.9838 0.0068
MCC Threshold 0.496 N/A
MCC 0.8564 N/A
F-score Threshold 0.496 N/A
F-score 0.932 N/A

Downloads

R Model Object

Random Forest model object (.RData)

Download RData

Positive Set

SMILES string + affinity value (.tsv)

Download TSV


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Page generated on: 2014-04-29 14:39:47