Efficient synthesis of trypsin inhibitor SFTI-1 via intramolecular ligation of peptide hydrazide

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• 作者：Yi-Qun Chen^a ; ^b ; Chen-Chen Chen^b ; Yao He^c ; Mu Yu^c ; Lin Xu^d ; Chang-lin Tian^c ; Qing-Xiang Guo^d ; Jing Shi^d ; ; Min Zhang^a ; ; Yi-Ming Li^b ; ^{lym2007@mail.ustc.edu.cn" class="auth_mail}
• 关键词：Cyclic peptides ; Protein chemical synthesis ; SFTI-1 ; Peptide hydrazides
• 刊名：Tetrahedron Letters
• 出版年：23 April, 2014
• 年：2014
• 卷：55
• 期：17
• 页码：2883-2886
• 全文大小：1044 K

文摘

Cyclic peptide trypsin inhibitor SFTI-1 was synthesized via intramolecular ligation of a linear peptide hydrazide with high yield. This cyclization strategy did not cause epimerization at the C-terminal Arg residue. CD spectrum and NMR spectroscopy analysis demonstrated that well-folded SFTI-1 could be obtained via standard oxidative folding process. Thus, we present a simple and cost-efficient strategy for the synthesis of SFTI-1.