Department of Chemistry, The University of Hong Kong, Hong Kong, People's Republic of China.
Proc Natl Acad Sci U S A. 2013 Apr 23;110(17):6657-62. doi: 10.1073/pnas.1221012110. Epub 2013 Apr 8.
An efficient method has been developed for the salicylaldehyde ester-mediated ligation of unprotected peptides at serine (Ser) or threonine (Thr) residues. The utility of this peptide ligation approach has been demonstrated through the convergent syntheses of two therapeutic peptides--ovine-corticoliberin and Forteo--and the human erythrocyte acylphosphatase protein (∼11 kDa). The requisite peptide salicylaldehyde ester precursor is prepared in an epimerization-free manner via Fmoc-solid-phase peptide synthesis.
现已开发出一种有效的方法，可通过水杨醛酯介导在丝氨酸（Ser）或苏氨酸（Thr）残基处连接未保护的肽。该肽连接方法的实用性已通过两种治疗性肽——羊促皮质素和福替奥——以及人红细胞酰基磷酸酶蛋白（约 11 kDa）的收敛性合成得到证明。所需的肽水杨醛酯前体可通过 Fmoc 固相肽合成以无差向异构化的方式制备。
