兰州大学机构库
One New Acid-Activated Hybrid Anticancer Peptide by Coupling with a Desirable pH-Sensitive Anionic Partner Peptide
Chang, Linlin1,2,3; Wu, Xiaoyan1,2,3; Ran, Kaixin1,2,3; Tian, Yali1,2,3; Ouyang, Xu1,2,3; Liu, Hui1,2,3; Gou, Sanhu1,2,3; Zhang, Yun1,2,3; Ni, Jingman1,2,3
2023-02
Online publication date2023-02
Source PublicationACS Omega   Impact Factor & Quartile
ISSN2470-1343
AbstractAnticancer peptides (ACPs) are promising antitumor resources, and developing acid-activated ACPs as more effective and selective antitumor drugs would represent new progress in cancer therapy. In this study, we designed a new class of acid-activated hybrid peptides LK-LE by altering the charge shielding position of the anionic binding partner LE based on the cationic ACP LK and investigated their pH response, cytotoxic activity, and serum stability, in hoping to achieve a desirable acid-activatable ACP. As expected, the obtained hybrid peptides could be activated and exhibit a remarkable antitumor activity by rapid membrane disruption at acidic pH, whereas its killing activity could be alleviated at normal pH, showing a significant pH response compared with LK. Importantly, this study found that the peptide LKLE3 with the charge shielding in the N-terminal of LK displayed notably low cytotoxicity and more stability, demonstrating that the position of charge masking is extremely important for the improvement of peptide toxicity and stability. In short, our work opens a new avenue to design promising acid-activated ACPs as potential targeting agents for cancer treatment.
PublisherAMER CHEMICAL SOC
DOI10.1021/acsomega.2c06766
Indexed BySCIE
Language英语
WOS Research AreaChemistry
WOS SubjectChemistry, Multidisciplinary
WOS IDWOS:000934570500001
Original Document TypeArticle ; Early Access
PMID 36873017
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttps://ir.lzu.edu.cn/handle/262010/499692
Collection兰州大学
Corresponding AuthorZhang, Yun; Ni, Jingman
Affiliation1.Lanzhou Univ, Chinese Acad Med Sci, Res Unit Peptide Sci, 2019RU066, Lanzhou 730000, Peoples R China;
2.Lanzhou Univ, Inst Pharmaceut, Sch Pharm, Lanzhou 730000, Peoples R China;
3.Lanzhou Univ, Sch Basic Med Sci, Key Lab Preclin Study New Drugs Gansu Prov, Lanzhou 730000, Peoples R China
Recommended Citation
GB/T 7714
Chang, Linlin,Wu, Xiaoyan,Ran, Kaixin,et al. One New Acid-Activated Hybrid Anticancer Peptide by Coupling with a Desirable pH-Sensitive Anionic Partner Peptide[J]. ACS Omega,2023.
APA Chang, Linlin.,Wu, Xiaoyan.,Ran, Kaixin.,Tian, Yali.,Ouyang, Xu.,...&Ni, Jingman.(2023).One New Acid-Activated Hybrid Anticancer Peptide by Coupling with a Desirable pH-Sensitive Anionic Partner Peptide.ACS Omega.
MLA Chang, Linlin,et al."One New Acid-Activated Hybrid Anticancer Peptide by Coupling with a Desirable pH-Sensitive Anionic Partner Peptide".ACS Omega (2023).
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