TargetNet


Q14790

Caspase-8


Function

Most upstream protease of the activation cascade of caspases responsible for the TNFRSF6/FAS mediated and TNFRSF1A induced cell death. Binding to the adapter molecule FADD recruits it to either receptor. The resulting aggregate called death- inducing signaling complex (DISC) performs CASP8 proteolytic activation. The active dimeric enzyme is then liberated from the DISC and free to activate downstream apoptotic proteases. Proteolytic fragments of the N-terminal propeptide (termed CAP3, CAP5 and CAP6) are likely retained in the DISC. Cleaves and activates CASP3, CASP4, CASP6, CASP7, CASP9 and CASP10. May participate in the GZMB apoptotic pathways. Cleaves ADPRT. Hydrolyzes the small-molecule substrate, Ac-Asp-Glu-Val-Asp-|-AMC. Likely target for the cowpox virus CRMA death inhibitory protein. Isoform 5, isoform 6, isoform 7 and isoform 8 lack the catalytic site and may interfere with the pro-apoptotic activity of the complex.


Database Links

Database Links
UniProt Q14790
PDB 1F9E, 1I4E, 1QDU, 1QTN, 2C2Z, 2FUN, 2K7Z, 2Y1L, 3H11, 3KJN, 3KJQ, 4JJ7
BioGrid 107291
BindingDB Q14790
DrugBank Not available
Guide to PHARMACOLOGY 1624
PharmGKB PA26092
KEGG hsa:841
BioCyc Not available
Entrez Gene (GeneID) 841

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.9567 0.004
Accuracy 0.9016 0.0056
Sensitivity 0.9127 0.0094
Specificity 0.8919 0.0059
BEDROC 0.9701 0.0084
MCC Threshold 0.39 N/A
MCC 0.8237 N/A
F-score Threshold 0.39 N/A
F-score 0.9083 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 14:39:48