磷酸化血管紧张素Ⅱ的合成及性质

Synthesis and Characterization of Phosphoangiotensin Ⅱ

蛋白质磷酸化和去磷酸化几乎调节着生命活动的所有过程, 包括细胞的增殖发育和分化、神经活动、肌肉收缩、新陈代谢和肿瘤发生等[1], 而磷肽则是体现其母体蛋白磷酸化过程结构变化的最好模型[2]. 磷肽合成的常用方法是将合成好的未被磷酸化的多肽与ATP在磷酸激酶的作用下进行酶法磷酸化, 但是该法对于不能被磷酸激酶磷酸化的多肽并不适用. 迄今为止, 磷肽及其类似物的化学合成仍非轻而易举之事[3,4].

Abstract The reversible phosphorylation/dephosphorylation of protein is probably the most common andimportant regulatory modification of proteins. Synthesis and identification of phosphopeptide have beenshown to have dramatic agonist effects in several signaling pathways. The phosphoangiotensin I was syn-thesized with two different strategies: global approach and building block approach. The building block ap-proach using phosphorylation regeants di-tert-butyl-N,N-diethyl phosphoramidite is the preferred methodfor the synthesis of peptides containing phosphotyrosine. The phosphoangiotensin and angiotensin were easily distinguished by ESI-MS. It may be useful to determining the phosphrylation sites of peptidescontaining multi-phosphorylated tyrosines by multi-stage mass. The phosphorylation of angiotensin I de-creases the content of-helix and increases the contents of -turn.