DSPE-PEG-ALD在肽药物N-末端特异性偶联中的应用-UDP糖丨MOF丨金属有机框架丨聚集诱导发光丨荧光标记推荐西安齐岳生物

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DSPE-PEG-ALD在肽药物N-末端特异性偶联中的应用

发布时间：2025-07-09 作者：zyl 分享到：

文献：Dual Functioned Pegylated Phospholipid Micelles Containing Cationic Antimicrobial Decapeptide for Treating Sepsis

作者：Wonhwa Lee 1,*, Eun Ji Park 1,*, Gahee Min 1, Joonhyeok Choi 1, Dong Hee Na 1,#, Jong-Sup Bae 1

文献链接：https://pmc.ncbi.nlm.nih.gov/articles/PMC5667346/

PEGylation is an effective approach for improving the therapeutic efficacy of peptide drugs by increasing their systemic circulation time, and by improving their stability in biological fluids 19-21. PEG-aldehyde (PEG-ALD) or DSPE-PEG-aldehyde (DSPE-PEG-ALD) site-specifically reacts with the N-terminal amine of KSLW under acidic conditions 22 based on the difference in the reactivity of the α-amino group at the N-terminus (pKa = 7.6-8.0), and ε-amino group in the Lys residue (pKa = 10.0-10.2) 23. In the present study, KSLW was modified using a PEG-ALD or was conjugated with DSPE-PEG-ALD. Fig. 1A shows the reaction between KSLW and DSPE-PEG-ALD, which forms a secondary amine linkage between PEG and the N-terminal amine of KSLW. Because DSPE-PEG has a low CMC of approximately 1 μM because of the requirement of strong hydrophobic driving forces for inducing self-assembly 24, KSLW reacts with the surface of these micelles (Fig. 1B). Average molecular masses of PEG-KSLW and PLM-KSLW, which were measured by performing matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS), were 7,246.8 and 5,660.2 Da, respectively (Fig. 1C), indicating that the mono-PEGylation reaction was complete in both PEG-KSLW and PLM-KSLW.

聚乙二醇化是通过增加肽药物的体循环时间和提高其在生物体液中的稳定性来提高肽药物治疗效果的有效方法。

基于N-末端α-氨基（pKa=7.6-8.0）和Lys残基中ε-氨基（pKa=10.0-10.2）23的反应性差异，PEG醛（PEG-ALD）或DSPE-PEG醛（DSPE-PEG-ALD）位点在酸性条件下与KSLW的N-末端胺特异性反应22。在本研究中，KSLW使用PEG-ALD进行改性或与DSPE-PEG-ALD偶联。

显示了KSLW和DSPE-PEG-ALD之间的反应，该反应在PEG和KSLW的N端胺之间形成仲胺键。由于诱导自组装需要强大的疏水驱动力，DSPE-PEG的CMC约为1μM，因此KSLW与这些胶束的表面发生反应。

通过基质辅助激光解吸/电离飞行时间质谱（MALDI-TOF MS）测量的PEG-KSLW和PLM-KSLW的平均分子质量分别为7246.8和5660.2 Da，表明PEG-KSLW和PLM-KSLW中的单聚乙二醇化反应都是完全的。