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Target intelligence / Profile preview
Tumor Protein p53 (Mutated) (p53 (Mutated))
- Target
- p53 (Mutated)
- Molecular classification
- Transcription factor, Tumor suppressor
01
Overview
Mutated p53 protein, resulting from mutations in the TP53 gene, is a dysfunctional form of the p53 tumor suppressor. These mutations commonly occur within the DNA-binding domain, leading to loss-of-function, dominant-negative, or gain-of-function effects. Mutant p53 impairs cell cycle checkpoints and apoptosis, promoting cancer development. Certain mutant forms exhibit oncogenic activities. Therapeutic strategies aim to restore wild-type function or eliminate harmful mutant activities.
- Other names
- Mutant p53TP53 (Mutated)
02
Mechanism of action
Restoration of wild-type p53 function, Inhibition of mutant p53 function, Targeted degradation of mutant p53
03
Biological functions
Cell cycle regulationApoptosisDNA repairCellular stress responseTranscriptional regulationOncogenesis (Gain-of-function mutants)
04
Disease associations
CancerLi-Fraumeni syndrome
05
Safety considerations
Off-target effectsDrug resistanceComplexity of targeting diverse p53 mutationsPotential for paradoxical effects (e.g., activating mutant p53 with undesirable consequences)
06
Interacting drugs
APR-246 (Eprenetapopt)
4 more in the full profile.
07
Biomarkers
p53 mutation statusp53 protein expression levelDownstream target gene expressionChemoresistancePrognosis
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