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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:
文献资料 :Dual Functioned Pegylated Phospholipid Micelles Containing Cationic Antimicrobial Decapeptide for Treating Sepsis我:Wonhwa Lee 1,*, Eun Ji Park 1,*, Gahee Min 1, Joonhyeok Choi 1, Dong Hee Na 1,#, Jong-Sup Bae 1资料联结:


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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聚乙二醇化是实现添加肽性类药物的体反复的时间和从而增长其在海洋生物品液中的稳明确高性来从而增长肽性类药物手术治疗功能的有用手段。对于N-下端α-氨基(pKa=7.6-8.0)和Lys残基中ε-氨基(pKa=10.0-10.2)23的生理的反应性能差异,PEG醛(PEG-ALD)或DSPE-PEG醛(DSPE-PEG-ALD)位点在呈酸性能力下与KSLW的N-下端胺特女性朋友生理的反应22。在本探析中,KSLW安全使用PEG-ALD来增韧或与DSPE-PEG-ALD偶联。显示信息了KSLW和DSPE-PEG-ALD区间内的表现,该表现在PEG和KSLW的N端胺区间内达成仲胺键。致使介导自主装须要强硬的疏水驱动安装力,DSPE-PEG的CMC约为1μM,所以说KSLW与某些胶束的单单从表面出现表现。凭借产品助手激光器解吸/电离起飞精力质谱(MALDI-TOF MS)量测的PEG-KSLW和PLM-KSLW的平衡分子结构水平区分为7246.8和5660.2 Da,取决于PEG-KSLW和PLM-KSLW中的单聚乙二醇化影响都要几乎的。涉及到安利: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不低于好文章网站内容因素当下杂志或参考文献,如遇图片侵权请联络我们公司删掉!