Issue 7, 2021

C-Terminal lactamization of peptides

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.

Graphical abstract: C-Terminal lactamization of peptides

Supplementary files

Article information

Article type
Communication
Submitted
07 Sept. 2020
Accepted
14 Dec. 2020
First published
16 Dec. 2020

Chem. Commun., 2021,57, 895-898

C-Terminal lactamization of peptides

N. H. Fischer, D. S. Nielsen, D. Palmer, M. Meldal and F. Diness, Chem. Commun., 2021, 57, 895 DOI: 10.1039/D0CC06018F

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