ArticleCancer discovery2025
Restoration of the Tumor Suppressor Function of Y220C-Mutant p53 by Rezatapopt, a Small-Molecule Reactivator.
Article in Cancer discovery, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed.
- Article
- A breakthrough in p53-targeted therapy.Nature cancer · 2026Article
- Design, synthesis and network pharmacology-integrated evaluation of benzenesulfonamides as potential Dickkopf-1 (Dkk-1)-targeting anticancer candidates.RSC advances · 2026Article
- Personalized medicine, scientific revolution or self-serving illusion: viewpoint from EORTC-PAMM Group.ESMO open · 2026Review
- Pleomorphism in Soft Tissue Sarcomas: Molecular Characteristics and Clinical Features.Medical sciences (Basel, Switzerland) · 2026Review
- Associative memory plays a role in ER-1α positive breast cancers.Cell death and differentiation · 2026Review
- Fragility of precision: resistance to mutant p53 reactivation.Signal transduction and targeted therapy · 2026Article
- DNA-contact mutant p53 displaces BRCA2 from chromatin and drives R-loop-associated genome instability.Genome biology · 2026Article
- A Roadmap to Transform Lung Cancer Outcomes: Priorities in Biology, Therapeutic Innovation, Early Detection, Prevention, and Interception.Cancer discovery · 2026Review
- Covalent drug rescue of multiple p53 mutants by stabilizing vinyl sulfone fragments hints to a specific refolding mechanism for R282W.Protein science : a publication of the Protein Society · 2026Article
- Molecular Characterization ofCancers · 2026Article
- The evolving global landscape of first-in-class oncology drug innovation.Signal transduction and targeted therapy · 2026Review
- Activating p53Nature communications · 2026Article
- Hijacking mutant p53 abundance.Nature chemical biology · 2026Article
- Molecularly Targeted Therapies in Oncology: Mechanisms, Resistance, and Combination Strategies.Molecules (Basel, Switzerland) · 2026Review
- Acquired On-Target Alterations Drive Clinical Resistance to p53-Y220C Reactivators.Cancer discovery · 2026Article
- Targeting mutant p53 in cancer: from mechanistic insights to therapeutic strategies.Cellular & molecular biology letters · 2026Review
- Dual Targeting of Mutant p53 and SNRPD2 via Engineered Exosomes Modulates Alternative Splicing to Suppress Ovarian Cancer.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Targeting the p53 cancer mutants Y220C, Y220N, and Y220S with the small-molecule stabilizer rezatapopt.Cell death & disease · 2026Article
- Tumor genomics in patients younger than 40 years of age with metastatic breast cancer.NPJ precision oncology · 2026Article
Corrections and comments
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Authors and funding
29 authors.
Funding
Abstract
Restoration of the tumor suppressor function of tumor-associated p53 mutants, including the Y220C substitution, has posed a significant challenge for therapeutic discovery. In this study, we describe rezatapopt (PC14586), part of a series of compounds designed to reactivate the p53 Y220C mutant. These compounds restore p53 tumor suppressor function by correcting its conformation and enabling it to bind DNA and activate downstream target genes, thus inducing antiproliferative changes in tumor cells. Our findings are supported by biochemical and structural analysis, in vitro and in vivo transcriptomics, and functional data, revealing the recovery of multiple aspects of the wild-type p53 program. These compounds demonstrate potent antitumor activity in preclinical models as single agents and in combination with immunotherapy. Currently, rezatapopt is being evaluated in a registrational phase II clinical trial for patients with advanced solid tumors harboring the TP53 Y220C mutation. SIGNIFICANCE: Rezatapopt is a clinical-stage compound that offers a promising treatment option for TP53-mutant cancers. This study details the characterization of rezatapopt and its related compounds, which can reinstate the tumor suppressor activity of the p53 Y220C mutant. These results emphasize the potential for targeting p53 mutations in cancer therapy.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.