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Structural studies and cyclization of the neuroprotective octapeptide NAPVSIPQ to improve cell permeability
Peptide Science ( IF 1.5 ) Pub Date : 2020-07-11 , DOI: 10.1002/pep2.24179 Dawn Ernenwein 1 , Sarah E. St. John 1 , Alistair J. Stewart 2 , Bruce H. Morimoto 2 , Jean Chmielewski 1 , Mark A. Lipton 1
Peptide Science ( IF 1.5 ) Pub Date : 2020-07-11 , DOI: 10.1002/pep2.24179 Dawn Ernenwein 1 , Sarah E. St. John 1 , Alistair J. Stewart 2 , Bruce H. Morimoto 2 , Jean Chmielewski 1 , Mark A. Lipton 1
Affiliation
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A secondary structural model for the neuroprotective octapeptide NAPVSIPQ in DMSO was developed using a combination of NMR spectroscopy and molecular dynamics simulations. On the basis of this model, four cyclized analogues of NAPVSIPQ were designed to improve its cell permeability with a long‐term view to oral delivery and increasing central nervous system (CNS) penetration. Testing of cell permeability through a monolayer of Caco‐2 cells demonstrated that three of the four cyclized analogues did exhibit up to 5‐fold improved permeability through the Caco‐2 monolayer. Additionally, none of the peptides appears to be P‐glycoprotein substrates subject to cellular efflux.
中文翻译：
神经保护性八肽NAPVSIPQ的结构研究和环化以提高细胞通透性
结合NMR光谱学和分子动力学模拟，开发了DMSO中神经保护性八肽NAPVSIPQ的二级结构模型。在此模型的基础上，设计了NAPVSIPQ的四个环化类似物以提高其细胞通透性，从长远角度来看口服给药和增加中枢神经系统（CNS）渗透。通过单层Caco-2细胞的细胞通透性测试表明，四个环化类似物中的三个确实表现出通过Caco-2单层的通透性提高了5倍。此外，这些肽都不是受细胞外排作用的P-糖蛋白底物。
更新日期：2020-07-11
中文翻译：
神经保护性八肽NAPVSIPQ的结构研究和环化以提高细胞通透性
结合NMR光谱学和分子动力学模拟，开发了DMSO中神经保护性八肽NAPVSIPQ的二级结构模型。在此模型的基础上，设计了NAPVSIPQ的四个环化类似物以提高其细胞通透性，从长远角度来看口服给药和增加中枢神经系统（CNS）渗透。通过单层Caco-2细胞的细胞通透性测试表明，四个环化类似物中的三个确实表现出通过Caco-2单层的通透性提高了5倍。此外，这些肽都不是受细胞外排作用的P-糖蛋白底物。
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