INSERM U836, Grenoble Neuroscience Institute, Site Santé La Tronche, Chemin Fortuné Ferrini, BP 170, 38042 Grenoble Cedex 9, France; Université Joseph Fourier, 38041 Grenoble, France.
INSERM UMR1097, Luminy, 13288 Marseille, France.
J Biol Chem. 2012 May 18;287(21):17331-17342. doi: 10.1074/jbc.M112.360628. Epub 2012 Mar 20.
Maurocalcine is the first demonstrated example of an animal toxin peptide with efficient cell penetration properties. Although it is a highly competitive cell-penetrating peptide (CPP), its relatively large size of 33 amino acids and the presence of three internal disulfide bridges may hamper its development for in vitro and in vivo applications. Here, we demonstrate that several efficient CPPs can be derived from maurocalcine by replacing Cys residues by isosteric 2-aminobutyric acid residues and sequence truncation down to peptides of up to 9 residues in length. A surprising finding is that all of the truncated maurocalcine analogues possessed cell penetration properties, indicating that the maurocalcine is a highly specialized CPP. Careful examination of the cell penetration properties of the truncated analogues indicates that several maurocalcine-derived peptides should be of great interest for cell delivery applications where peptide size matters.
Maurocalcine 是第一个被证实具有高效细胞穿透特性的动物毒素肽。尽管它是一种高效的细胞穿透肽(CPP),但其相对较大的 33 个氨基酸大小和三个内部二硫键的存在可能会阻碍其在体外和体内应用的发展。在这里,我们证明通过用等排 2-氨基丁酸残基替换 Cys 残基,并将序列截断至多达 9 个残基的长度,可以从 maurocalcine 中衍生出几种有效的 CPP。一个令人惊讶的发现是,所有截断的 maurocalcine 类似物都具有细胞穿透特性,这表明 maurocalcine 是一种高度特化的 CPP。对截断类似物的细胞穿透特性的仔细研究表明,一些源自 maurocalcine 的肽应该对肽大小很重要的细胞递药应用非常有兴趣。