Lim, Dhi Vya and Woo, Wei Hwei and Lim, Jing Xuan and Loh, Xin Yee and Soh, Hui Ting and Lim, Seng Yung Adrian and Lee, Zheng Yang and Yow, Hui Yin and Hamzah, Sharina Binti and Sellappans, Renukha and Foo, Jhi Biau (2024) Targeting mutant-p53 for cancer treatment: Are we there yet? Current Molecular Pharmacology, 17. ISSN 1874-4672, DOI https://doi.org/10.2174/1874467217666230914090621.
Full text not available from this repository.Abstract
Background: Mutations in the TP53 gene are the most common among genetic alterations in human cancers, resulting in the formation of mutant p53 protein (mutp53). Mutp53 promotes proliferation, migration, invasion, and metastasis in cancer cells. Not only does the initiation of oncogenesis ensue due to mutp53, but resistance towards chemotherapy and radiotherapy in cancer cells also occurs. This review aims to summarise and discuss the oncogenesis of mutant p53 in cancer cells and introduce the various mutant p53 inhibitors currently being evaluated at the pre-clinical and clinical stages. Compounds that induce the wild-type conformation on the targeted p53 missense mutation, restore or enhance the DNA binding of mutant p53, and inhibit cancer cells' growth are highlighted. In addition, the progression and development of the mutant p53 inhibitors in clinical trials are updated. Conclusion: The progress of developing a cancer treatment that may successfully and efficiently target mutant p53 is on the verge of development. Mutant p53 proteins not only initiate oncogenesis but also cause resistance in cancer cells to certain chemo or radiotherapies, further endorse cancer cell survival and promote migration as well as metastasis of cancerous cells. With this regard, many mutant p53 inhibitors have been developed, some of which are currently being evaluated at the pre-clinical level and have been identified and discussed. To date, APR-246 is the most prominent one that has progressed to the Phase III clinical trial. © 2024 The Author(s).
| Item Type: | Article |
|---|---|
| Funders: | Taylor’s University |
| Uncontrolled Keywords: | Cancer; Chemo or radiotherapies; Clinical; Inhibitors; mutp53; Oncogenesis; p53; Preclinical |
| Subjects: | R Medicine R Medicine > RM Therapeutics. Pharmacology |
| Divisions: | Faculty of Pharmacy > Department of Pharmaceutical Life Sciences |
| Depositing User: | Ms. Juhaida Abd Rahim |
| Date Deposited: | 16 Apr 2024 07:06 |
| Last Modified: | 16 Apr 2024 07:06 |
| URI: | http://eprints.um.edu.my/id/eprint/44987 |
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