突变体
癌变
癌症研究
癌症
癌细胞
生物
转移
错义突变
突变
基因
遗传学
作者
Dmitry Lim,Wei Hwei Woo,Jing Xuan Lim,Xin Yi Loh,Heun Soh,Su Yin Lim,Zheng Yang Lee,Hui-Yin Yow,Sharina Hamzah,Renukha Sellappans,Jhi Biau Foo
出处
期刊:Current Molecular Pharmacology
[Bentham Science]
日期:2023-11-03
卷期号:17
被引量:1
标识
DOI:10.2174/1874467217666230914090621
摘要
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.
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