Méry J, Granier C, Juin M, Brugidou J
Research Centre for Macromolecular Biochemistry, CNRS, Montpellier, France.
Int J Pept Protein Res. 1993 Jul;42(1):44-52. doi: 10.1111/j.1399-3011.1993.tb00348.x.
The use of disulfide bonds for peptide-resin linkage in solid-phase peptide synthesis was investigated using polyacrylic polymers (Expansin) and automated Fmoc methodology. The disulfide moiety was bound to the support either by coupling a protected bifunctional handle or by an original stepwise procedure. Among the three different disulfide handles that were investigated, only the aminoethyldithio-2-isobutyric acid (AEDI) handle was stable enough to achieve peptide synthesis. A series of peptides of up to 10-20 amino acids were prepared in this manner, in good yield and purity. Rapid and quantitative peptide release was obtained by reduction with equimolecular amounts of dithiothreitol at pH 9 or tris(2-carboxymethyl) phosphine at pH 4.5. This allowed direct and rapid coupling of the released cysteamide peptides to an activated protein carrier and the use of free or resin-bound forms of the antigen in immunoassays.
使用聚丙烯酸聚合物（膨胀素）和自动化Fmoc方法研究了二硫键在固相肽合成中用于肽-树脂连接的情况。二硫部分通过连接受保护的双功能手柄或通过原始的逐步程序与载体结合。在所研究的三种不同的二硫手柄中，只有氨基乙基二硫代-2-异丁酸（AEDI）手柄足够稳定以实现肽合成。以这种方式制备了一系列多达10-20个氨基酸的肽，产率和纯度良好。通过在pH 9下用等分子数量的二硫苏糖醇或在pH 4.5下用三（2-羧甲基）膦还原，可实现快速和定量的肽释放。这允许将释放的半胱胺肽直接快速偶联到活化的蛋白质载体上，并在免疫测定中使用游离或树脂结合形式的抗原。
