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| Main Authors: | , , |
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| Format: | Artículo Open Access |
| Published: |
Wiley
2025
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| Subjects: | |
| Online Access: | https://onlinelibrary.wiley.com/doi/10.1002/psc.70012 |
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Table of Contents:
- Structural Modification and Antitumor Activity Study of Peptide Codesane: Discovery of Novel Stapled Peptide Antitumor Agents Qingmei Li Lijuan Qiu Yong Li Journal of Peptide Science ABSTRACTThe discovery of novel candidate molecules that may transform cancer treatment carries significant clinical implications. Codesane (COD), an 18‐amino acid peptide extracted from the wild bee venom of Colletes daviesanus, is categorized as a cationic α‐helical amphipathic antimicrobial peptide. COD, produced via solid‐phase peptide synthesis, displayed significant antitumor activity in vitro. However, its application as a drug is restricted by conformational flexibility, poor serum stability, and low selectivity. This research focused on designing, synthesizing, and evaluating a series of stapled COD derivatives by all‐hydrocarbon stapling strategy. Compared to the original peptide COD, several of these stapled derivatives showed significant enhancements in α‐helicity, serum resistance, antitumor activity, and cell selectivity. Significantly, the stapled derivative COD‐5, which possesses high helicity, good serum stability, and favorable selectivity, shows promising potential for novel antitumor drug development, whereas COD‐3, characterized by high selectivity and good antitumor activity, serves as a preferred candidate for novel breast cancer therapeutic drugs. These findings provide a solid foundation for developing innovative and highly effective antitumor therapies. 10.1002/psc.70012 http://onlinelibrary.wiley.com/termsAndConditions#vor