Total Synthesis and Structural Characterization of Caveolin-1
Total Synthesis and Structural Characterization of Caveolin-1
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DOI：
10.1002/anie.202100826
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发表时间：
2021-05-11
影响因子：
16.6
通讯作者：
Hirabayashi, Yoshio
中科院分区：
文献类型：
--
作者：
Hojo, Hironobu;Takei, Toshiki;Hirabayashi, Yoshio
Caveolin-1是细胞膜小窝形成所必需的蛋白质。它由177个氨基酸残基组成，在C-末端区域三重棕榈酰化，并插入脂质双层以在多肽链中间形成V形结构。将整个序列分为五个肽段，每个肽段均通过固相法合成。为了提高C-末端区域的溶解度，引入O-酰基异肽结构。在通过硫酯方法连接并引入棕榈酰基后，除去所有保护基，并将异肽结构转化为天然肽键。最后，所获得的多肽被成功地插入到bicelles中，从而表明合成成功。
Caveolin-1, which is an essential protein for caveola formation, was chemically synthesized. It is composed of 177 amino acid residues, is triply palmitoylated at the C-terminal region, and is inserted into the lipid bilayer to form a V-shaped structure in the middle of the polypeptide chain. The entire sequence was divided into five peptide segments, each of which was synthesized by the solid-phase method. To improve the solubility of the C-terminal region, O-acyl isopeptide structures were incorporated. After ligation by the thioester method and the introduction of the palmitoyl groups, all the protecting groups were removed and the isopeptide structures were converted into the native peptide bond. Finally, the obtained polypeptide was successfully inserted into bicelles, thus showing the success of the synthesis.