您当前所在位置:首页 > 资讯信息 > 试剂课堂
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:
文献综述 :Dual Functioned Pegylated Phospholipid Micelles Containing Cationic Antimicrobial Decapeptide for Treating Sepsis作家:Wonhwa Lee 1,*, Eun Ji Park 1,*, Gahee Min 1, Joonhyeok Choi 1, Dong Hee Na 1,#, Jong-Sup Bae 1期刊论文下载链接:


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. 

Gso6k8KkkM7RycDaQNRv.png

聚乙二醇化是能够 提升了肽药的体循环法精力和提升了其在生物工程体液中的安全稳界定来提升了肽药手术治疗视觉效果的高效方法步骤。依据N-后部α-氨基(pKa=7.6-8.0)和Lys残基中ε-氨基(pKa=10.0-10.2)23的生理响应能力差异,PEG醛(PEG-ALD)或DSPE-PEG醛(DSPE-PEG-ALD)位点在酸碱性环境下与KSLW的N-后部胺特异形生理响应22。在本理论研究中,KSLW实用PEG-ALD采取热塑性树脂或与DSPE-PEG-ALD偶联。显视了KSLW和DSPE-PEG-ALD直接的表现,该表现在PEG和KSLW的N端胺直接构成仲胺键。是由于引发自拆装必须强硬的疏水推能量,DSPE-PEG的CMC约为1μM,那么KSLW与此类胶束的外壁会出现表现。能够机质外挂缴光解吸/电离着陆时长质谱(MALDI-TOF MS)在测量的PEG-KSLW和PLM-KSLW的均原子水平各为7246.8和5660.2 Da,阐明PEG-KSLW和PLM-KSLW中的单聚乙二醇化想法基本都是充分的。想关强烈推荐: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及以上小文章內容来历各种各样论文期刊或文章,如果有侵权行为请找话题自己误删!