Douat Céline, Heitz Annie, Paris Marielle, Martinez Jean, Fehrentz Jean-Alain
Laboratoire des Amino-acides, Peptides et Protéines, UMR 5810, Faculté de Pharmacie, Universités Montpellier I et II, 34093 Montpellier Cédex 5, France.
J Pept Sci. 2002 Nov;8(11):601-14. doi: 10.1002/psc.420.
A new strategy for the synthesis of lipopeptides has been developed. Using Weinreb (N-methoxy, N-methyl) amide as an aldehyde function precursor on the side chains of Asp or Glu residues, this new strategy avoids the synthesis of a lipidic amino acid residue before its incorporation in the peptide sequence. The aldehyde generated on the solid support can react with ylides leading to unsaturated or saturated side chains or with various nucleophiles to yield non-coded amino acid residues incorporated into the sequence.
一种合成脂肽的新策略已被开发出来。利用Weinreb(N-甲氧基,N-甲基)酰胺作为天冬氨酸或谷氨酸残基侧链上醛基功能的前体,这种新策略避免了在将脂氨基酸残基并入肽序列之前进行其合成。在固相载体上生成的醛可以与叶立德反应生成不饱和或饱和侧链,或者与各种亲核试剂反应,以产生并入序列中的非编码氨基酸残基。