A 37-residue peptide corresponding to the entire amino acid sequence of chicken calcitonin-gene-related peptide (cCGRP) was synthesized by successive assembling of seven peptide fragments via the azide, followed by acid treatments of protected cCGRP in two steps, i.e., first with trifluoroacetic acid (TFA) in the presence of diphenylsulfide to establish the disulfide bond between the Cys(MBzl) sulfoxide and the Cys(MBzl) residues (positions 2 and 7, respectively) and then with 1 M trimethylsilyl trifluoromethanesulfonate in TFA to remove the rest of the protecting groups employed. The synthetic peptide suppressed the 45Ca release from mouse calvaria.
通过
叠氮化物连续组装七个肽片段,然后分两步对受保护的 cCGRP 进行酸处理,合成了对应于鸡
降钙素基因相关肽 (cCGRP) 整个
氨基酸序列的 37 个残基肽,即:在
二苯硫醚存在下与
三氟乙酸 (TFA) 反应,在 Cys(MBzl) 亚砜和 Cys(MBzl) 残基(分别为位置 2 和 7)之间建立二
硫键,然后与 TFA 中的 1 M 三甲基甲
硅烷基
三氟甲磺酸酯反应以除去使用其余的保护基团。合成肽抑制小鼠颅盖释放 45Ca。