点击将三价甘露糖基糖簇与人血清白蛋白偶联，生成细胞靶向递送载体。

IF 3 3区医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic & Medicinal Chemistry Pub Date : 2025-11-01 Epub Date: 2025-07-29 DOI:10.1016/j.bmc.2025.118335

Yu-Fan Zhou, Hui Xu, Dan-Yang Chen, Xi-Le Hu, Guo-Rong Chen, Tony D James, Xiao-Peng He

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引用次数: 0

摘要

利用聚糖作为靶向剂构建递送材料已被证明对靶向疾病的诊断和治疗是有用的。为了实现有效靶向，制备了多价糖苷来增强与糖受体的亲和力。在本研究中，我们设计并合成了一种新的三价甘露糖（Man3-PEG3-N3），带有一个叠氮基单元。该叠氮甘露糖基糖簇通过菌株促进的点击化学与环辛基修饰的人血清白蛋白（HSA）结合。质谱分析证实了糖簇共轭HSA的成功构建，荧光滴定试验表明所得到的共轭物能够容纳环境敏感的染料。

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Click conjugation of trivalent mannosyl glycocluster with human serum albumin to generate a cell targeting delivery vehicle.

The exploitation of glycans as targeting agents to construct delivery materials has proved useful for targeted disease diagnosis and therapy. To achieve effective targeting, multivalent glycosides are prepared to enhance avidity with sugar receptors. In this study, we designed and synthesized a new trivalent mannoside (Man₃-PEG₃-N₃) bearing an azido unit. This azido mannosyl glycocluster was used to conjugate with cyclooctyne-modified human serum albumin (HSA) through strain-promoted click chemistry. Mass spectroscopic analysis validated the successful construction of the glycocluster-conjugated HSA, and a fluorescence titration assay indicated that the resulting conjugate is capable of accommodating an environmentally sensitive dye.

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来源期刊

Bioorganic & Medicinal Chemistry 医学-生化与分子生物学

CiteScore

6.80

自引率

2.90%

发文量

413

审稿时长

17 days

期刊介绍： Bioorganic & Medicinal Chemistry provides an international forum for the publication of full original research papers and critical reviews on molecular interactions in key biological targets such as receptors, channels, enzymes, nucleotides, lipids and saccharides. The aim of the journal is to promote a better understanding at the molecular level of life processes, and living organisms, as well as the interaction of these with chemical agents. A special feature will be that colour illustrations will be reproduced at no charge to the author, provided that the Editor agrees that colour is essential to the information content of the illustration in question.