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p53 activators and inhibitors act on the tumor suppressor p53, a transcription factor activated by cellular stress. In unstressed cells the ubiquitin ligase mouse double minute 2 (MDM2) keeps p53 levels low by promoting its degradation. RG7112 blocks the p53-MDM2 interaction, and SJ 172550 targets the related protein mouse double minute 4 (MDM4, also called MDMX). RITA binds p53 itself, while tenovin-1 and tenovin-6 raise cellular p53 levels. Tenovin-6 also inhibits the deacetylases sirtuin 1 and sirtuin 2 (SIRT1, SIRT2). Pifithrin-α hydrobromide works the other way, inhibiting p53-dependent transcription in cells exposed to genotoxic stress. Further compounds directed at MDM2 are listed in the neighboring MDM2 category.
MIRA-1 restores wild-type conformation, function and DNA binding activity to mutant p53. Induces p53 transcriptional transactivation of p21, MDM2 and PUMA.
Synonyms: PC14586
Rezatapopt (PC14586) is a small-molecule ligand that specifically targets the mutated TP53 protein, particularly the Y220C variant. By binding to a unique pocket formed by this mutation, Rezatapopt restores the structural integrity and tumor suppressor functions of p53. This compound has shown promising antitumor activity, leading to tumor inhibition and regression in mouse models with established human tumor xenografts featuring the TP53 Y220C mutation, making it a valuable tool for cancer research targeting p53 dysfunction.
PK7242 is a potent inducer of mutant p53 reactivation, specifically targeting the p53-Y220C variant in cancer cells. This compound promotes growth inhibition, triggers cell-cycle arrest, and initiates apoptosis in tumor cells harboring the Y220C mutation. PK7242 is a valuable tool for investigating therapeutic strategies aimed at targeting p53 deficiencies in cancer research.
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