Huang Ye, Li Wang, Zhou Yuke, Bai Jinping, Li Ning, Su Zhengding, Cheng Xiyao
Institute of Modern Fermentation Engineering and Future Foods, School of Light Industry and Food Engineering, Guangxi University, No. 100, Daxuedong Road, Nanning 530004, China.
School of Pharmaceutical Sciences and Institute of Materia Medica, Xinjiang University, Urumqi 830017, China.
Cells. 2025 Apr 12;14(8):583. doi: 10.3390/cells14080583.
is a tumor suppressor gene and is regarded as one of the most crucial genes in protecting humans against cancer. The protein Mdm2 and its homolog MdmX serve as negative regulators of p53. In nearly half of cancer cells, there is an overexpression of Mdm2 and MdmX, which inhibit p53 activity. Furthermore, Mdm2's E3 ubiquitin ligase activity promotes the ubiquitination and degradation of p53. Therefore, blocking the interaction between p53 and Mdm2/MdmX to prevent the degradation of wild-type p53 is an effective strategy for inhibiting tumor growth. This paper primarily discusses the regulatory relationship between p53, MdmX and Mdm2, and provides a review of the current status of p53-Mdm2/MdmX inhibitors. It aims to offer a theoretical foundation and research direction for the future discovery and design of targeted inhibitors against the p53-Mdm2/MdmX interaction.
是一种肿瘤抑制基因，被认为是保护人类抵御癌症的最关键基因之一。蛋白质Mdm2及其同源物MdmX作为p53的负调节因子。在近一半的癌细胞中，Mdm2和MdmX存在过表达，抑制p53活性。此外，Mdm2的E3泛素连接酶活性促进p53的泛素化和降解。因此，阻断p53与Mdm2/MdmX之间的相互作用以防止野生型p53降解是抑制肿瘤生长的有效策略。本文主要讨论p53、MdmX和Mdm2之间的调节关系，并综述p53-Mdm2/MdmX抑制剂的现状。旨在为未来针对p53-Mdm2/MdmX相互作用的靶向抑制剂的发现和设计提供理论基础和研究方向。
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