Study on the design, synthesis and activity of MDM2/MDMX anti-tumor stapled peptide PROTAC
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X Liao, M Guo, D Hu, C Su, H Liao
Scientific Reports, 2025
nature.com
PROTAC is a drug development technology that uses the Ubiquitin-Proteasome System (UPS) to degrade target proteins, and enhances the degradation ability of target proteins through E3 ubiquitin ligase, which can further enhance the anti-tumor effect of targeted drug molecules. In this study, a series of dual-target MDM2/MDMX stapled peptide PROTAC based on SM3-4 were designed and synthesized, and the stapled peptide PROTAC DSM3-2 and DSM3-5 screened in the study inhibited tumor cell growth in vitro at low µM …
