Fmoc策略固相合成磷酰化肽研究进展

Progress on the synthesis of phosphopeptides by the Fmoc solid-phase strategy

蛋白质的磷酰化和去磷酰化对多种生命活动的调节起着关键的作用,磷酰化肽是研究这些生命调节过程中一类非常重要的物质。自20世纪40年代人类首次成功地合成出磷酰化肽以来,磷酰化肽的研究就引起了化学家和生物学家的广泛关注。由于Fmoc固相合成策略在多肽的合成中被普遍应用,因此,Fmoc固相合成策略也已经成为目前磷酰化肽最主要的合成手段。该文对近年来采用Fmoc固相合成策略进行磷酰化肽合成的方法(包括整体磷酰化法和磷酰化单体合成法)进行了总结,并对各种合成方法的优缺点进行了讨论。

Both protein phosphorylation and dephosphorylation play key roles in the regulation of a wide range of life activities.Phosphopeptides are very important compounds for the study of these processes.Since the first successful chemical synthesis in 1940′s,the phosphopeptides has attracted wide attention among chemists and biologists.The Fmoc solid phase synthesis strategy has become the main synthetic method for phosphopeptides.This article summarizes recent progress on Fmoc solid-phase synthesis strategy for phosphopeptides（including global phosphorylation and phosphorylation of building blocks）.The advantage and disadvantage of various synthetic methods are also discussed.