Selective Enzymatic Removal of Protecting Groups from Phosphopeptides: Chemoenzymatic Synthesis of a Characteristic Phosphopeptide Fragment of the Raf-1 Kinase
作者:Dagmar Sebastian
DOI:10.1055/s-1997-1306
日期:1997.9
Base-labile biologically relevant phosphopeptides can advantageously be synthesized under very mild conditions and without undesired side reactions by employing the heptyl (Hep) ester as C-terminal or the phenylacetamide (PhAc) as N-terminal enzyme-labile protecting group. The lipase-mediated saponification of the heptyl ester blocking function was successfully applied in the construction of a characteristic selectively phosphorylated hydroxyamino acid fragment of Raf-1 kinase, an important member of the so-called Ras signal transduction pathway.
The present invention relates to methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included. Compounds for use in these methods are provided, as are methods of identifying such compounds.