Study on the design, synthesis and activity of antitumor staple peptides targeting MDM2/MDMX Provisionally Accepted
Xiufei Liao- 1Tarim University, China
- 2Pidu District People's Hospital, China
- 3Chengdu Medical College, China
Staple peptides, which have a significantly enhanced pharmacological profile, are promising therapeutic molecules due to their remarkable resistance to proteolysis and cell-penetrating properties. In this study, we designed and synthesized a series of PMI-M3-based dual-targeting MDM2/MDMX staple peptides, and compared with the straight-chain peptides, the stapler peptide SM3-4 screened in the study induced apoptosis of tumor cells in vitro at low μM concentrations, and the helix was significantly increased. Studies have shown that the enhancement of staple activity is related to the increase of helicity, and SM3-4 provides an effective research basis for dual-targeted anti-tumor staple peptides.
Keywords: Stapled peptides, Double-targeted, anti-tumor, MDM2, MDMX
Received: 19 Mar 2024;
Accepted: 20 May 2024.
Copyright: © 2024 Liao, Yang, Hu, Mo, Gao and Liao. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Mr. Xiufei Liao, Tarim University, Aral, 843300, Xinjiang Uyghur Region, China