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Target intelligence / Profile preview
Proto-oncogene protein c-mdm2 (MDM2)
- Target
- MDM2
- Molecular classification
- E3 ubiquitin ligase, Oncoprotein
01
Overview
MDM2 is an important negative regulator of the tumor suppressor p53. It functions as an E3 ubiquitin ligase that mediates the polyubiquitination of p53, targeting it for proteasomal degradation and inhibiting its transcriptional activity. Overexpression or amplification of MDM2 is observed in various human tumors, contributing to oncogenesis. It also interacts with other proteins and participates in DNA repair pathways independently of its role as an E3 ligase. Small-molecule antagonists targeting the p53-MDM2 interaction are under development as cancer therapeutics.
- Other names
- E3 ubiquitin-protein ligase Mdm2Oncoprotein Mdm2Hdm2P53-binding proteinDouble minute 2 protein
02
Mechanism of action
Small-molecule antagonists bind within the N-terminal pocket used for interaction with p53, preventing this interaction and reactivating wild-type p53 function.
03
Biological functions
Negative regulation of p53UbiquitinationCell cycle regulationApoptosis regulationDNA repair modulation
04
Disease associations
CancerDedifferentiated liposarcoma
05
Safety considerations
Overexpression or amplification leads to functional suppression of wild-type TP53Inactivation of tumor-suppressive pathways
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