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Table 2 Inhibitors associated with blocking p53 aggregation

From: p53 amyloid aggregation in cancer: function, mechanism, and therapy

Inhibitor

Type

Targeting the p53 mutation site

Principle

Experiment

ReACp53[109]

A designed 17-residue peptide Inhibitor

Target R175 and R248 in HGSOC, have no effect on cells with folded wild-type p53

p53 amyloid spine structure is used to design ReACp53 ((R9)RPILTRITLE). Targeting p53 segment 251–257

In vitro and in vivo

LI [110]

Bifunctional ligands

Y220C

Zn-free p53 exhibits accelerated protein aggregation, and LI modulate mutant p53 aggregation and restore zinc binding using a metallochaperone approach

In vitro and in vivo

Tripyridylamide ADH-6[111]

Protein mimetic amyloid inhibitor

Target R175 and R248 in Pancreatic cancer, have no effect on cells with folded wild-type p53

α-Helix mimetics are small molecules that imitate the topography of the most commonly occurring protein secondary structure, serving as effective antagonists of protein–protein interactions (PPIs) at the interaction interface

In vitro and in vivo