Sandrine Sagan, Philippe Karoyan, Olivier Lequin, Gerard Chassaing and Solange Lavielle Pages 2799 - 2822 ( 24 )
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 restrictφ 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.
amino acid,n-methylation,methylation,organic synthesis,structure,backbone constraint,peptide,biological activity
, , , , UMR 7613 CNRSUniversite Pierre&Marie Curie, Structure and Function of Bioactive Molecules, Case courrier 182, 4 place Jussieu, 75005 Paris, France.