Sagan Sandrine, Karoyan Philippe, Lequin Olivier, Chassaing Gérard, Lavielle Solange
UMR 7613 CNRS-Université Pierre & Marie Curie, Structure and Function of Bioactive Molecules, Case courrier 182, 4 place Jussieu, 75005 Paris, France.
Curr Med Chem. 2004 Nov;11(21):2799-822. doi: 10.2174/0929867043364108.
Numerous backbone constraints can be used to develop pseudopeptides or pseudomimetics of biologically active peptides. Among those, N- and Calpha-methyl amino acids that can be incorporated by solid-phase peptide synthesis in a bioactive sequence represent important tools to restrict phi and psi angles of peptide backbone. This review will focus on the chemical syntheses of N- and Calpha-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.
众多的主链限制可用于开发生物活性肽的拟肽或拟态物。其中，可通过固相肽合成引入生物活性序列中的N-甲基和α-甲基氨基酸是限制肽主链φ角和ψ角的重要工具。本综述将聚焦于N-甲基和α-甲基氨基酸的化学合成、它们对肽构象和结构的影响，以及它们在肽对酶促降解的稳定性和所得类似物的生物活性方面所起的作用。
