Protein chemical synthesis by serine and threonine ligation.

Zhang, Yinfeng; Xu, Ci; Lam, Hiu Yung; Lee, Chi Lung; Li, Xuechen · Proc Natl Acad Sci U S A · 2013

basic_science · Level V

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Abstract

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.

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