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. 2024 Oct 24;55(1):7. doi: 10.3892/ijmm.2024.5448

Table I.

Therapeutic compounds changing mutant p53 conformation to wild-type-like structure that are under evaluation in clinical trials.

Agent Target Class Mechanism Phases of clinical trials Clinical trial nos.
APR-246 p53 R175H
p53 R273H
Small molecule Wild-type-like conformation of p53 by binding to thiol groups I-III NCT03072043, NCT03588078, NCT03745716, NCT04383938, NCT04419389, NCT03931291, NCT04214860
PEITC R175H
P223L
Phytochemical Wild-type-like conformation of p53, oxidative stress I-II NCT01790204, NCT03034603
PC14586 Y220C Small molecule Selectively restores wild-type p53 conformation I NCT04585750
ATO R175H
V272M
R282W
E285K
Y234C
Small molecule Restores wild-type p53 conformation I-II NCT03855371, NCT04489706, NCT04695223, NCT04869475
Sodium stibogluconate 65 mutants Pentavalent antimony compound Restores wild-type p53 conformation II NCT04906031
COTI2 R175H
R273H
R273C
R282W
Zn2+ chelator Inhibition of mutant p53 misfolding I NCT02433626