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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:
期刊论文 :Dual Functioned Pegylated Phospholipid Micelles Containing Cationic Antimicrobial Decapeptide for Treating Sepsis做者:Wonhwa Lee 1,*, Eun Ji Park 1,*, Gahee Min 1, Joonhyeok Choi 1, Dong Hee Na 1,#, Jong-Sup Bae 1期刊论文超链接:


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. 

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聚乙二醇化是完成增多肽类药物治療的体循环系统精力和提升其在怪物质液中的维持性来提升肽类药物治療治療郊果的管用方式。根据N-末段α-氨基(pKa=7.6-8.0)和Lys残基中ε-氨基(pKa=10.0-10.2)23的作用力差异,PEG醛(PEG-ALD)或DSPE-PEG醛(DSPE-PEG-ALD)位点在强酸状况下与KSLW的N-末段胺活性朋友作用22。在本探索中,KSLW操作PEG-ALD做好渗透型或与DSPE-PEG-ALD偶联。体现了KSLW和DSPE-PEG-ALD左右的生理体现,该生理体现在PEG和KSLW的N端胺左右进行仲胺键。因分析自制做要有强大的的疏水驱动安装力,DSPE-PEG的CMC约为1μM,所以KSLW与等胶束的表明进行生理体现。依据产品外挂脉冲光解吸/电离飞机飞行日子质谱(MALDI-TOF MS)侧量的PEG-KSLW和PLM-KSLW的分別团伙产品品质区别为7246.8和5660.2 Da,表达PEG-KSLW和PLM-KSLW中的单聚乙二醇化现象皆是非常的。有关系个性化推荐:DSPE-PEG-AldDSPE-PEG-Amine,1069-79-0DSPE-PEG-azideDSPE-PEG5-azideDSPE-PEG-BiotinDSPE-PEG-BoronateDSPE-PEG-CH2COOHDSPE-PEG-COOHDSPE-PEG-Cy3DSPE-PEG-Cy5DSPE-PEG-DBCODSPE-PEG-FITC以上的稿件的内容源特殊学术期刊或论文参考文献,要是有图片侵权请找你们删除图片!