Cardona V M F, Hartley O, Botti P
Department of Medical Biochemistry, University Medical Center, Geneva, Switzerland.
J Pept Res. 2003 Mar;61(3):152-7. doi: 10.1034/j.1399-3011.2003.00043.x.
A new method to cyclize unprotected peptides is presented. The method involves the use of a 1-phenyl-2-mercaptoethyl derivative on the N-terminal glycine. This template acts as an auxiliary thiol-containing group in order to drive cyclization with a counterpart thioester moiety on the same molecule. Subsequent facile removal of the derivative generates products with only native peptide structure. The successful, high-yield cyclization of the peptide GSPYSSDTTPA is described.
本文介绍了一种环化未保护肽的新方法。该方法涉及在N端甘氨酸上使用1-苯基-2-巯基乙基衍生物。该模板作为含辅助硫醇的基团,以便与同一分子上的对应硫酯部分驱动环化反应。随后轻松去除该衍生物,生成仅具有天然肽结构的产物。文中描述了肽GSPYSSDTTPA成功的高产率环化反应。