肽的 C 端内酰胺化。

C-Terminal lactamization of peptides.

机构信息

Center for Evolutionary Chemical Biology, Department of Chemistry, University of Copenhagen, Universitetsparken 5, Copenhagen 2100, Denmark.

出版信息

Chem Commun (Camb). 2021 Jan 28;57(7):895-898. doi: 10.1039/d0cc06018f.

DOI:10.1039/d0cc06018f

PMID:33367306

Abstract

Solid-phase synthesis of peptides (SPPS) with release through formation of C-terminal γ-, δ-, or ε-lactams is presented. The natural products ciliatamide A and C were synthesized in up to 90% yield. Peptides carrying C-terminal lactams were shown to possess increased bio-stability and comparable biological activity as compared to the parent non-lactamized peptide amides.

摘要

通过形成 C 末端 γ-、δ-或 ε-内酰胺来进行肽的固相合成（SPPS）被提出。天然产物 ciliatamide A 和 C 的合成产率高达 90%。与母体非内酰胺化的肽酰胺相比，携带 C 末端内酰胺的肽具有更高的生物稳定性和相当的生物活性。