Proteins play important roles in living organisms, such as involving in metabolism for maintaining the essential function and participating in a variety of biological pathways. Therefore, understanding of its biological function, location and binding associates becomes an very important issue for advanced studies. However, the instability as well as low expression level makes certain important proteins very difficult to be collected. Therefore, peptide synthesis and peptide ligation may promise an avenue for preparing those polypeptide chains with reasonable yields and purity. In this review, we try to introduce the background of peptide synthesis and further extend to recent progress of peptide-peptide ligations.