三种优化的检测方法，用于评估可拯救 p53 突变体的化合物。
Three optimized assays for the evaluation of compounds that can rescue p53 mutants.
机构信息
Shanghai Institute of Hematology, State Key Laboratory of Medical Genomics, National Research Center for Translational Medicine (Shanghai), Ruijin Hospital affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China.
出版信息
STAR Protoc. 2021 Jul 27;2(3):100688. doi: 10.1016/j.xpro.2021.100688. eCollection 2021 Sep 17.
Identifying drugs targeting p53 remains a major focus of precision oncology, with over twenty compounds that can rescue p53 mutants reported. Here, we suggest three easily accessible assays to determine the thermostability, protein folding, and transcriptional activity of p53 mutants-the go-to criteria for evaluating a rescue compound that acts by increasing p53 thermostability. Because of the diversity of p53 mutants, a compound that meets the criteria of one assay does not necessarily meet the criteria of the other assays. For complete details on the use and execution of this protocol, please refer to Chen et al. (2021).
鉴定针对 p53 的药物仍然是精准肿瘤学的主要重点，已有超过二十种能够挽救 p53 突变体的化合物被报道。在这里，我们建议三种易于获得的测定法来确定 p53 突变体的热稳定性、蛋白质折叠和转录活性——这是评估通过增加 p53 热稳定性发挥作用的挽救化合物的首选标准。由于 p53 突变体的多样性，符合一种测定法标准的化合物不一定符合其他测定法的标准。有关此方案使用和执行的完整详细信息，请参阅 Chen 等人（2021 年）。
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