Thioamide ligations: new technologies for peptide and protein synthesis

本项目旨在开发用于多肽和蛋白质化学合成的新型酰胺键形成反应。利用最近发现的银促进的硫代酰胺偶联反应，将开发新的肽连接策略，包括基于天冬酰胺的连接和不依赖残基的连接。还将开发一种新的后期、化学选择性的多肽和蛋白质中N-糖基化天冬酰胺残基的组装。这项研究的成果将导致多肽和蛋白质组装和功能化的合成方法的突破，从而使人们能够通过全化学合成获得一系列同质的、翻译后修饰的蛋白质。这些研究成果将扩大澳大利亚在生物技术领域的研究能力和全球竞争力，为澳大利亚第三大制造业带来重大好处。

This project aims to develop novel amide-bond forming reactions for the chemical synthesis of peptides and proteins. New peptide ligation strategies, including an asparagine-based ligation and a residue-independent ligation will be developed that exploit the recent discovery of silver-promoted coupling reactions of thioamides. A novel late-stage, chemo-selective assembly of N-glycosylated asparagine residues in peptides and proteins will also be developed. The outcomes of this research will lead to breakthroughs in synthetic methodologies for the assembly and functionalisation of peptides and proteins, thereby enabling access to a range of homogeneous, post translationally modified proteins though total chemical synthesis. These research outcomes will expand Australia's research capability and global competitiveness in the field of biotechnology, delivering significant benefits to the third largest manufacturing sector in Australia.