Restoration of the Tumor Suppressor Function of Y220C-Mutant p53 by Rezatapopt, a Small-Molecule Reactivator
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.
Authors
- Kimberly A. Robell
- Jonathan D. Oliner
- Brandon M. Russo
- Masha V. Poyurovsky (ORCID: https://orcid.org/0000-0002-3024-778X)
- Shunbin Xiong (ORCID: https://orcid.org/0000-0003-3984-1774)
- Melissa L. Johnson (ORCID: https://orcid.org/0000-0001-9874-1314)
- Anna M. Puzio‐Kuter
- Hongju H. Li
- Mary Kate McBrayer
- Bruce J. Fahr
- Dafydd H. Thomas (ORCID: https://orcid.org/0009-0006-0175-9416)
- Romyr Dominique
- Benjamin D. Greenbaum (ORCID: https://orcid.org/0000-0001-6153-8793)
- Josh Battaglia
- Kuo‐Sen Huang
- Guillermina Lozano (ORCID: https://orcid.org/0000-0001-8985-4886)
- Binh T. Vu
- Alison M. Schram (ORCID: https://orcid.org/0000-0002-6070-2413)
- Melissa Dumble
- Alyssa M. Brown
- Arnold J. Levine (ORCID: https://orcid.org/0000-0002-1871-6387)
- Amy E. Wiebesiek
- Hong Yang (ORCID: https://orcid.org/0009-0007-5871-6852)
- Peirong Yang
- Marc Fellous
- Lizhong Xu
- Chris L. Mulligan
- Thomas W. Davis
- Alexander Solovyov (ORCID: https://orcid.org/0000-0002-7682-4706)
Institutions
- Amgen (United States) (US)
- Memorial Sloan Kettering Cancer Center (US)
- The University of Texas MD Anderson Cancer Center (US)
- Princeton University (US)
- Kettering University (US)
- Institute for Advanced Study (US)
- Sarah Cannon (US)
- Nutrasource (CA)
- Tennessee Oncology (US)
Publication Details
- Journal
- Cancer Discovery
- Published
- 2025-02-13
- DOI
- https://doi.org/10.1158/2159-8290.cd-24-1421
- Citations
- 33
- Primary Topic
- Cancer-related Molecular Pathways
- Type
- article
- Field-Weighted Citation Impact
- 34.50
Funders
- National Cancer Institute