N- and Cα-Methylation in Biologically Active Peptides: Synthesis, Structural and Functional Aspects
Abstract:Numerous backbone constraints can be used to develop pseudopeptides or pseudomimetics of biologically active peptides. Among those, N- and Cα-methyl amino acids that can be incorporated by solidphase peptide synthesis in a bioactive sequence represent important tools to restrict and ψ angles of peptide backbone.
This review will focus on the chemical syntheses of N- and Cα-methyl amino acids, their effects on peptide conformation and structure, and their role on the peptide stability towards enzymatic degradation and on the biological activities of the resulting analogues.
Document Type: Review Article
Affiliations: UMR 7613 CNRSUniversite Pierre & Marie Curie, Structure and Function of Bioactive Molecules, Case courrier 182, 4 place Jussieu, 75005 Paris, France.
Publication date: November 1, 2004
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