一类多肽偶联药物及其制备方法和应用

By designing peptide-conjugated drugs, AIP-IIID4A amide cyclic peptides are linked to antibiotics to achieve bacterial targeting and release of high concentrations of antibiotics intracellularly. This solves the problem that existing antibiotics cannot clear intracellular bacteria and has the advantages of simplified synthesis and reduced immunogenicity.

CN119701000BActive Publication Date: 2026-07-17FOURTH MILITARY MEDICAL UNIVERSITY

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FOURTH MILITARY MEDICAL UNIVERSITY
Filing Date
2024-12-25
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing antibiotics are ineffective at eliminating intracellular infections of Staphylococcus aureus, leading to drug resistance and increased patient burden with long-term use. Existing drug delivery strategies suffer from poor targeting specificity and immunogenicity issues.

Method used

A peptide-conjugated drug was designed, using AIP-IIID4A amide cyclic peptide as a target, which was linked to an antibiotic via click chemistry. The linker arm was specifically hydrolyzed in the lysosome, achieving bacterial targeting and releasing high concentrations of antibiotics intracellularly.

Benefits of technology

It achieves co-localization of antibiotics and bacteria within cells, efficiently eliminates intracellular bacteria, simplifies drug synthesis, reduces the risk of immunogenicity, and has good antibacterial effects.

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Abstract

本发明公开了一类多肽偶联药物及其制备方法和应用,属于生物医药技术领域,本发明所述多肽偶联药物由环肽分子、连接臂、间隔子及抗生素类药物通过化学键键合连接而成;环肽分子选择AIP‑III D4A酰胺及其结构类似物;连接臂选择对溶酶体中组织蛋白酶B特异性敏感的分子;间隔子为可自行降解的结构片段。本发明的多肽偶联药物具有良好的抗菌效果,尤其对目前临床治疗中较为棘手的胞内菌感染具有突出的治疗效果,可用于制备高效的抗菌药物。
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