Diaminodiacid-based solid-phase synthesis of all-hydrocarbon stapled α-helical peptides
作者:Feng-Liang Wang、Ye Guo、Si-Jian Li、Qing-Xiang Guo、Jing Shi、Yi-Ming Li
DOI:10.1039/c5ob00741k
日期:——
Fmoc-solid phase peptide synthesis (SPPS) that employed pre-prepared diaminodiacid building blocks to introduce all-hydrocarbon staples into peptides by on-resin cyclization. Compared to unstapled native peptides, diaminodiacid-based stapled peptides exhibited an increased α-helicity ratio and stability toward protease. Moreover, the linkage length was found to affect the bioactivity of the peptides and their
本文中描述了使用Fmoc-固相肽合成(SPPS)的另一种装订策略,所述Fmoc-固相肽合成采用预先制备的二氨基二酸结构单元通过树脂上的环化作用将全碳氢化合物短肽引入肽中。与未装订的天然肽相比,基于二氨基二酸的装订肽表现出增加的α-螺旋比和对蛋白酶的稳定性。此外,发现连接长度影响肽的生物活性及其抑制Wnt途径的能力。因此,新的装订方法提供了另一种方法来获得具有可调的二氨基二酸接头的装订肽。