TargetNet


Q00987

E3 ubiquitin-protein ligase Mdm2


Function

E3 ubiquitin-protein ligase that mediates ubiquitination of p53/TP53, leading to its degradation by the proteasome. Inhibits p53/TP53- and p73/TP73-mediated cell cycle arrest and apoptosis by binding its transcriptional activation domain. Also acts as a ubiquitin ligase E3 toward itself and ARRB1. Permits the nuclear export of p53/TP53. Promotes proteasome-dependent ubiquitin-independent degradation of retinoblastoma RB1 protein. Inhibits DAXX-mediated apoptosis by inducing its ubiquitination and degradation. Component of the TRIM28/KAP1-MDM2-p53/TP53 complex involved in stabilizing p53/TP53. Also component of the TRIM28/KAP1-ERBB4-MDM2 complex which links growth factor and DNA damage response pathways. Mediates ubiquitination and subsequent proteasome degradation of DYRK2 in nucleus. Ubiquitinates IGF1R and SNAI1 and promotes them to proteasomal degradation.


Database Links

Database Links
UniProt Q00987
PDB 1RV1, 1T4E, 1T4F, 1YCR, 1Z1M, 2AXI, 2C6A, 2C6B, 2F1Y, 2FOP, 2GV2, 2HDP, 2LZG, 2M86, 2VJE, 2VJF, 3EQS, 3G03, 3IUX, 3IWY, 3JZK, 3JZR, 3JZS, 3LBK, 3LBL, 3LNJ, 3LNZ, 3TJ2, 3TPX, 3TU1, 3V3B, 3VBG, 3VZV, 3W69, 4DIJ, 4ERE, 4ERF, 4HBM, 4HFZ, 4HG7, 4JV7, 4JV9, 4JVE, 4JVR, 4JWR, 4MDN, 4MDQ
BioGrid 110358
BindingDB Q00987
DrugBank Not available
Guide to PHARMACOLOGY Not available
PharmGKB PA30718
KEGG hsa:4193
BioCyc Not available
Entrez Gene (GeneID) 4193

Chemical Space of the Positive Compounds


Model Performance Metrics

Metric Mean Value Standard Deviation
AUC 0.8268 0.0099
Accuracy 0.72 0.0145
Sensitivity 0.7391 0.0136
Specificity 0.6974 0.0224
BEDROC 0.9876 0.0087
MCC Threshold 0.632 N/A
MCC 0.4948 N/A
F-score Threshold 0.304 N/A
F-score 0.7827 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 14:39:45