Target intelligence / Profile preview

Proto-oncogene protein MDM2 (MDM2)

Target
MDM2
Molecular classification
E3 ubiquitin ligase, Proto-oncogene
01

Overview

MDM2 is a nuclear-localized E3 ubiquitin-protein ligase that negatively regulates the tumor suppressor protein p53. It binds to p53, inhibiting its transcriptional activity and promoting its degradation. Overexpression or amplification of MDM2 is observed in various cancers, leading to reduced p53 function and uncontrolled cell proliferation. MDM2 also participates in DNA repair pathways independently of its E3 ligase activity.

Other names
p53-binding proteinRING-type E3 ubiquitin transferaseOncoprotein Mdm2
02

Mechanism of action

Inhibition of MDM2-p53 interaction, leading to p53 activation and subsequent cell cycle arrest or apoptosis.

03

Biological functions

Negative regulation of p53Protein ubiquitinationCell cycle regulationApoptosis regulationDNA repair
04

Disease associations

CancerAccelerated tumor formationDedifferentiated liposarcoma
05

Safety considerations

Potential for off-target effects due to broad interactionsDevelopment of resistance through alternative pathwaysToxicity associated with p53 activation in normal tissues
06

Biomarkers

MDM2 overexpressionMDM2 amplification

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