Design, Synthesis, and Biological Evaluation of Arginine <i>N</i>‑Glycosylation Stapled Peptides with Potent Antitumor Activity <i>In Vivo</i>

The host defense peptide PP-1 has attracted attention for its strong antitumor activity. However, its potential for clinical use is hindered by its poor proteolytic stability. In this study, a series of stapled PP-1 derivatives were obtained by an all-hydrocarbon stapling strategy and arginine <i...

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Bibliographic Details
Main Author:	Yinxue Fu (20681503) (author)
Other Authors:	Chunhui Dou (22289084) (author), Xiaoyang Gao (150076) (author), Shanping Ji (8975354) (author), Xuemei Zhao (10933) (author), Jingwen Xue (3808165) (author), Hao Yang (328526) (author), Nannan Song (5491205) (author), Chunyu Zhang (118320) (author), Changlong Wang (1915549) (author), Yulei Li (6287450) (author)
Published:	2025
Subjects:	Biochemistry Microbiology Cell Biology Physiology Pharmacology Ecology Immunology Cancer Biological Sciences not elsewhere classified Chemical Sciences not elsewhere classified superior cell permeability significantly weakened hemolysis peptide libraries containing nude mouse model hydrocarbon stapling strategy flow cytometry revealed confocal microscopy revealed strong antitumor activity potent antitumor activity lead antitumor agent poor proteolytic stability low hemolytic toxicity >- glycosylated peptides 60 holds promise 60 exhibited superior 60 could exert parent peptide pp antitumor effects antitumor activities serum stability >- glycosylation 60 stapled 60 displayed vivo </ vitro </ stapled pp rationally constructed potential toxicity n </ liver tissue inducing apoptosis five rounds clinical use biological evaluation attracted attention
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Design, Synthesis, and Biological Evaluation of Arginine <i>N</i>‑Glycosylation Stapled Peptides with Potent Antitumor Activity <i>In Vivo</i>

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