抑制器
平方毫米
P53蛋白
癌症研究
突变体
行动方式
细胞周期检查点
癌症
小分子
细胞周期
生物
计算生物学
细胞生物学
细胞凋亡
遗传学
生物化学
基因
作者
Maryam Fallatah,Fiona V. Law,Warren Chow,Peter Kaiser
标识
DOI:10.1016/j.tips.2023.02.007
摘要
The tumor suppressor p53 is the most frequently mutated protein in human cancer and tops the list of high-value precision oncology targets. p53 prevents initiation and progression of cancer by inducing cell-cycle arrest and various forms of cell death. Tumors have thus evolved ways to inactivate p53, mainly by TP53 mutations or by hyperactive p53 degradation. This review focuses on two types of p53 targeting compounds, MDM2 antagonists and mutant p53 correctors. MDM2 inhibitors prevent p53 protein degradation, while correctors restore tumor suppressor activity of p53 mutants by enhancing thermodynamic stability. Herein we explore both novel and repurposed p53 targeting compounds, discuss their mode of action, and examine the challenges in advancing them to the clinic.
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