Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden.
Cancer Discov. 2023 May 4;13(5):1043-1045. doi: 10.1158/2159-8290.CD-23-0229.
In this issue of Cancer Discovery, Adams and colleagues present the discovery of a potent PROTAC, MDM2 degrader, which activates wild-type p53 leading to cancer cell death. Importantly, in a number of in vitro and in vivo experiments, the authors show that the depletion of MDM2 by PROTAC kills p53-mutant or p53-null cancer cells. See related article by Adams et al., p. 1210 (5).
在本期《癌症发现》杂志中,Adams 及其同事报告了一种强效 PROTAC,即 MDM2 降解剂的发现,该降解剂能激活野生型 p53,导致癌细胞死亡。重要的是,在许多体外和体内实验中,作者表明,PROTAC 耗尽 MDM2 可杀死 p53 突变或 p53 缺失的癌细胞。请参阅 Adams 等人的相关文章,第 1210 页(5)。