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Target intelligence / Profile preview
Mouse Double Minute 2 Homolog (MDM2)
- Target
- MDM2
- Molecular classification
- E3 ubiquitin ligase, Oncoprotein, RING finger protein
01
Overview
Mouse double minute 2 homolog (MDM2) is an E3 ubiquitin ligase and a major negative regulator of the tumor suppressor p53. It inhibits p53's transcriptional activity and promotes its degradation. MDM2 is overexpressed or amplified in various cancers, making it a promising therapeutic target. Beyond cancer, MDM2 also plays a role in regulating immune responses and cardiovascular functions.
- Other names
- E3 ubiquitin-protein ligase Mdm2Hdm2
02
Mechanism of action
MDM2 inhibitors bind to MDM2, disrupting its interaction with p53, leading to p53 stabilization and activation of its downstream targets, inducing cell cycle arrest and/or apoptosis.
03
Biological functions
p53 regulationUbiquitinationCell cycle regulationApoptosis regulationTranscriptional regulationDNA repairDifferentiationTreg function modulationCardiovascular function regulation
04
Disease associations
CancerAutoimmune diseases
05
Safety considerations
Potential for off-target effects due to MDM2's interactions with other proteinsDevelopment of resistance to MDM2 inhibitorsOn-target toxicities related to p53 activation in normal tissues
06
Biomarkers
MDM2 expression levels in tumor tissuep53 status
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