Bioorganic Chemistry, University of Bayreuth, Universitätsstraße 30, Bayreuth, 95447, Germany.
J Pept Sci. 2021 Jan;27(1):e3283. doi: 10.1002/psc.3283. Epub 2020 Sep 3.
A convergent synthesis for erythropoietin (EPO) 1-28 N-glycopeptide hydrazides was developed. In this approach, EPO 1-28 peptides were synthesized on the solid phase and converted to C-terminal hydrazides after cleavage from the resin. After selective deprotection of the Asp24 side chain, the desired glycosylamine was coupled by pseudoproline-assisted Lansbury aspartylation. Although the initial yields of the EPO 1-28 glycopeptides were satisfactory, they could be markedly improved by increasing the purity of the peptide using a reversed-phase high-performance liquid chromatography (RP-HPLC) purification of the protected peptide.
开发了一种促红细胞生成素（EPO）1-28 N-糖肽酰肼的汇聚合成方法。在该方法中，EPO 1-28 肽在固相上合成，并在从树脂上裂解后转化为 C 末端酰肼。在 Asp24 侧链选择性脱保护后，通过拟脯氨酸辅助 Lansbury 天冬氨酸酰化反应偶联所需的糖基胺。尽管 EPO 1-28 糖肽的初始产率令人满意，但通过使用反相高效液相色谱（RP-HPLC）对保护肽进行纯化来提高肽的纯度，可以显著提高它们的产率。
