Target intelligence / Profile preview

Tumor protein p53 (Y220C mutant) (p53 Y220C)

Target
p53 Y220C
Molecular classification
Transcription factor
01

Overview

The tumor protein p53 (Y220C mutant) is a mutated form of the p53 tumor suppressor protein. The Y220C mutation, where tyrosine at position 220 is replaced by cysteine, destabilizes the protein and creates a unique druggable pocket. This loss-of-function mutation impairs p53's ability to bind DNA and activate genes involved in cell cycle arrest and apoptosis, promoting cancer development. It's found in approximately 1-1.8% of cancers. Therapeutic strategies focus on stabilizing the mutant protein with small molecules like H3 compound and Rezatapopt to restore its wild-type function.

Other names
TP53 Y220Cp53-Y220C mutantY220C p53
02

Mechanism of action

Small molecule stabilization of mutant p53 conformation; restoration of wild-type p53 function

03

Biological functions

Cell cycle regulationApoptosisDNA repairTumor suppression
04

Disease associations

CancerOvarian cancerLung cancerBreast cancerEndometrial cancer
05

Safety considerations

Potential for off-target effects of small molecule stabilizersDevelopment of resistance to targeted therapies
06

Interacting drugs

H3 compound

1 more in the full profile.

07

Biomarkers

TP53 Y220C mutation

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