Institute of Human Virology and Department of Biochemistry and Molecular Biology, University of Maryland School of Medicine, Baltimore, MD 21201, USA.
Curr Pharm Des. 2011;17(6):603-9. doi: 10.2174/138161211795222577.
The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the p53 tumor suppressor, directly contributing to the development and progression of many tumors harboring wild type p53. Antagonizing MDM2 and MDMX to activate the p53 pathway has thus become an attractive new strategy for anticancer drug design. Several different classes of MDM2 and MDMX antagonists have been reported, including low molecular weight compounds, small peptides, miniature proteins, and peptidomimetics. This review aims to summarize the latest progress in the design of peptide activators of the p53 tumor suppressor.
癌蛋白 MDM2 和 MDMX 负调控 p53 肿瘤抑制因子的活性和稳定性,直接促进许多携带野生型 p53 的肿瘤的发生和发展。因此,拮抗 MDM2 和 MDMX 以激活 p53 途径已成为一种有吸引力的抗癌药物设计新策略。已经报道了几种不同类型的 MDM2 和 MDMX 拮抗剂,包括低分子量化合物、小肽、微型蛋白和肽模拟物。本文旨在总结 p53 肿瘤抑制因子肽激活剂设计的最新进展。