Table 1.
Agents that target TP53 mutation.
| Compound | Mechanism | References |
| PRIMA-1 | restore the wild-type conformation to mutant P53 and induce apoptosis in cancer cells | (128) |
| APR-246(PRIMA-1Met) | restore the wild-type conformation to mutant P53 and induce apoptosis in cancer cells | (129, 130) |
| reduce glutathione(GSH) and thioredoxin reductase 1 (TXNRD1) | ||
| increase ROS levels | ||
| COTI-2 | promote refolding of mutant p53 and restore wild-type-p53 function | (124, 131) |
| lead to activation of AMPK and inhibit the PI3K-AKT pathway | ||
| MIRA1 | restore transcriptional transactivation to mutant p53 in living cells | (132) |
| STIMA-1 | preferentially kill mutant p53‐carrying tumor cells | (133) |
| activate caspases and induces Bax, PUMA and p21 | ||
| Zinc metallochaperone-1 (ZMC1/NSC319726) | activate mutant p53 by restoring proper zinc loading | (134, 135) |
| decrease cellular GSH levels and increase ROS levels | ||
| PK11007 and other similar compounds(PK11000,PK11010,PK11029,PK11003,PK11012 and PK11015) | alkylation of surface-exposed cysteines 182 and 277 and stabilized the p53 DBD without impairing its DNA-binding affinity | (126) |
| increase protein and mRNA levels of the p21 and PUMA | ||
| decrease cellular GSH levels and increase ROS levels | ||
| ReACp53 and related peptides(CDB3) | disrupts mutant-p53 aggregates and stabilise wild-type conformation | (136–138) |
| CP-31398 | protect p53 from thermal degeneration,restore the wild type function of some mutant p53 and up-regulate p53 levels | (139, 140) |
| PhiKan083(PK083) | Binds to the DNA-binding domain of mutant-p53 and restore the wild type function of some mutant p53 | (141–143) |
| RETRA | Treatment of mutant p53-expressing cancer cells with RETRA results in a substantial increase in the expression level of p73 | (144) |
| PC14586 | stabilize the Y220C mutant and restore p53 wild-type (normal) conformation | (145) |
| MDM2 Inhibitor:Nutlin-3 and ALRN-6924 | Increase p53 levels and activity | (146, 147) |
| RG7388 and AMG232 | disrupt the p53-MDM2 protein–protein interaction and prevent p53 from proteasomal degradation | (148, 149) |