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Fluorinated Modification as a Simple Strategy That Effectively Enhances the Stability and Activity of Antimicrobial
Xu Ouyang1, Liru Yuan1, Tingting Yang1
1Institute of Pharmaceutics, School of Pharmacy, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, and Research Unit of Peptide Science, Chinese Academy of Medical Sciences, 2019RU066, Lanzhou University, Lanzhou 730000, P. R. China.
Journal of Medicinal Chemistry
|September 29, 2025
Summary
Fluorination enhances antimicrobial peptides (AMPs) by improving stability and efficacy. A modified AMP, FuK, shows superior serum half-life and therapeutic potential, overcoming limitations of traditional AMPs.
Area of Science:
- Biochemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Antimicrobial peptides (AMPs) show promise as antibacterial agents but face challenges like proteolytic degradation and toxicity.
- The previously identified AMP, WK2, exhibits good antimicrobial activity but lacks stability for clinical use.
Purpose of the Study:
- To enhance the stability and antimicrobial properties of the AMP WK2.
- To investigate the structure-activity relationships of modified AMP analogs, specifically fluorinated versions.
Main Methods:
- Computer-based prediction of proteolytic cleavage sites in WK2.
- Modification of WK2 sequence with unnatural amino acids, focusing on fluorination.
- Systematic evaluation of enzymatic hydrolysis stability, antimicrobial activity, and cytotoxicity of novel analogs.
Main Results:
- The fluoropeptide analog, FuK, demonstrated significantly improved antibacterial properties compared to WK2.
- FuK exhibited a serum half-life exceeding 1440 minutes, over 6.4 times longer than WK2.
- In vivo studies confirmed FuK's excellent safety profile and therapeutic efficacy.
Conclusions:
- Fluorination modification is a promising strategy to enhance the antimicrobial properties and stability of AMPs.
- FuK represents a potential therapeutic candidate for bacterial infections, overcoming the limitations of native AMPs.
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