Chemical Synthesis of Proteins Through Native Chemical Ligation of Peptide Hydrazides

Since it was first reported that peptide hydrazides can be directly used for native chemical ligation, it has enabled the synthesis of cyclic peptides and proteins containing more than 300 amino acids. In this chapter, we start with the development of hydrazide in peptide chemistry, and then discuss the concept and optimization strategy of hydrazide-based native chemical ligation, including the preparation of peptide hydrazides, activation methods of peptide hydrazides, multiple fragment ligation. We also survey recent progress and applications in peptide drugs and protein synthesis.