C-Terminal lactamization of peptides. Issue 7 (24th December 2020)

• Record Type: Journal Article
• Authors: Fischer, Niklas H.; Nielsen, Daniel S.; Palmer, Daniel; Meldal, Morten; Diness, Frederik
• Is Part Of: Chemical communications. Volume 57:Issue 7(2021)
• Page Start: 895
• Page End: 898
• Publication Date: 2020-12-24
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc06018f
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : New solid-phase based methods have allowed efficient synthesis of natural products and novel peptide hormone derivatives with a C-terminal lactam. 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.