Toward Fully Synthetic Glycoproteins by Ultimately Convergent Routes: A Solution to a Long-Standing Problem
作者:J. David Warren、Justin S. Miller、Stacy J. Keding、Samuel J. Danishefsky
DOI:10.1021/ja0491836
日期:2004.6.1
A method is disclosed for the convergent synthesis of multiply glycosylated peptides. The approach centers on a convergent technique for generating masked, complex glycopeptide-containing C-terminal acyl donors. Activation of the latent donor in situ and use directly in segment coupling with a second peptide bearing a complex carbohydrate produces a completely unprotected, bifunctional glycopeptide
公开了一种用于多重糖基化肽的会聚合成的方法。该方法的中心是用于生成掩蔽的、复杂的含糖肽的 C 端酰基供体的收敛技术。原位激活潜在供体并直接用于与带有复杂碳水化合物的第二个肽偶联的片段,产生完全不受保护的双功能糖肽。该系统在完全收敛的片段偶联过程中,在酰基供体的 C 端氨基酸残基处显示出最低水平的水解和差向异构化,因此是合成糖蛋白的有力工具。