Gesellschaft zur Förderung der Analytischen Wissenschaften e.V., ISAS - Leibniz Institute for Analytical Sciences, Otto-Hahn-Str. 6b, D-44227 Dortmund, Germany, Tel: (+49)231-1392 4215.
Beilstein J Org Chem. 2012;8:804-18. doi: 10.3762/bjoc.8.90. Epub 2012 May 30.
Over the past few years, synthetic methods for the preparation of complex glycopeptides have been drastically improved. The need for homogenous glycopeptides and glycoproteins with defined chemical structures to study diverse biological phenomena further enhances the development of methodologies. Selected recent advances in synthesis and applications, in which glycopeptides or glycoproteins serve as tools for biological studies, are reviewed. The importance of specific antibodies directed to the glycan part, as well as the peptide backbone has been realized during the development of synthetic glycopeptide-based anti-tumor vaccines. The fine-tuning of native chemical ligation (NCL), expressed protein ligation (EPL), and chemoenzymatic glycosylation techniques have all together enabled the synthesis of functional glycoproteins. The synthesis of structurally defined, complex glycopeptides or glyco-clusters presented on natural peptide backbones, or mimics thereof, offer further possibilities to study protein-binding events.
在过去的几年中，复杂糖肽的制备合成方法得到了极大的改进。为了研究各种生物现象，需要具有明确化学结构的同质糖肽和糖蛋白，这进一步促进了方法学的发展。本文综述了糖肽或糖蛋白作为生物研究工具的合成和应用方面的最新进展。在合成基于糖肽的抗肿瘤疫苗的过程中，人们已经意识到针对聚糖部分以及肽骨架的特异性抗体的重要性。天然化学连接（NCL）、表达蛋白连接（EPL）和化学酶糖基化技术的精细调整都使得功能性糖蛋白的合成成为可能。在天然肽骨架上呈现的结构确定的、复杂的糖肽或糖簇，或其类似物的合成，为研究蛋白结合事件提供了进一步的可能性。
