The DOI matches its Crossref record; 13 of the 13 references it cites were found in a registry or an index.
Mutant p53 reactivation by small molecules makes its way to the clinic
Abstract
The TP53 tumor suppressor gene is mutated in many human tumors, including common types of cancer such as colon and ovarian cancer. This illustrates the key role of p53 as trigger of cell cycle arrest or cell death upon oncogenic stress. Most TP53 mutations are missense mutations that result in single amino acid substitutions in p53 and expression of high levels of dysfunctional p53 protein. Restoration of wild type p53 function in such tumor cells will induce robust cell death and allow efficient eradication of the tumor. Therapeutic targeting of mutant p53 in tumors is a rapidly developing field at the forefront of translational cancer research. Various approaches have led to the identification of small molecules that can rescue mutant p53. These include compounds that target specific p53 mutations, including PK083 and PK5174 (Y220C mutant p53) and NSC319726 (R175H mutant p53), as well as PRIMA‐1 and its analog APR‐246 that affect a wider range of mutant p53 proteins. APR‐246 has been tested in a Phase I/II clinical trial with promising results.
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“Therefore, targeting the hydrophobic pocket of Y220C becomes an ideal drug target, helping p53 to restore normal folding without interfering with p53 binding to DNA.466”
From Targeting p53 pathways: mechanisms, structures, and advances in therapy (2023) · cites this paper as [466]
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Cited by
Targeting p53 pathways: mechanisms, structures, and advances in therapy
Wang, H., Guo, M., Wei, H., & Chen, Y. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01347-1 · Cited by 1,016
Targeting mutant p53 for efficient cancer therapy
Bykov, V. J. N., Eriksson, S. E., Bianchi, J., & Wiman, K. G. (2018) · Nature Reviews Cancer · doi:10.1038/nrc.2017.109 · Cited by 889
Self-citationThe role of p53 in cancer drug resistance and targeted chemotherapy
Hientz, K., Mohr, A., Bhakta-Guha, D., & Efferth, T. (2017) · Oncotarget · doi:10.18632/oncotarget.13475 · Cited by 587
Therapeutic targeting of p53: all mutants are equal, but some mutants are more equal than others
Sabapathy, K., & Lane, D. P. (2018) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2017.151 · Cited by 517
SF3B1 mutation identifies a distinct subset of myelodysplastic syndrome with ring sideroblasts
Malcovati, L., Karimi, M., Papaemmanuil, E., Ambaglio, I., Jädersten, M., Jansson, M., Elena, C., Gallì, A., Walldin, G., Della Porta, M. G., et al. (2015) · Blood · doi:10.1182/blood-2015-03-633537 · Cited by 434
Metadata
- Authors
- Bykov, V. J. N., & Wiman, K. G.
- Venue
- FEBS Letters
- Publisher
- Wiley
- Published
- 2014-04-24
- Volume
- 588
- Issue
- 16
- Pages
- 2622-2627
- ISSN
- 0014-5793
- 1873-3468
- Cited by
- 162
- References
- 13
- Language
- en
- Funders
- Swedish Cancer Society
- Swedish Research Council
- EU FP6 Framework Program
- Radiumhemmets Forskningsfonder
- StratCan
- Stockholms Läns Landsting
- Karolinska Institutet
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