Ligation, Macrocyclization, and Simultaneous Functionalization of Peptides by Multicomponent Reactions (MCR)

Autor: Manuel G. Ricardo, Ludger A. Wessjohann, Aldrin V. Vasco, Daniel G. Rivera
Rok vydání: 2021
Předmět:
Zdroj: Methods in Molecular Biology ISBN: 9781071616888
Popis: Multicomponent reactions (MCRs) are recently expanding the plethora of solid-phase protocols for the synthesis and derivatization of peptides. Herein, we describe a solid-phase-compatible strategy based on MCRs as a powerful strategy for peptide cyclization and ligation . We illustrate, using Gramicidin S as a model peptide, how the execution of on-resin Ugi reactions enables the simultaneous backbone N-functionalization and cyclization, which are important types of derivatizations in peptide-based drug development or for incorporation of conjugation handles, or labels.
Databáze: OpenAIRE