The invention relates to methods for selectively converting a cysteine residue in a peptide or protein to the dehydroalanine (Dha) residue. The method also works on selenocysteine and substituted cysteine and selenocysteine residues, resulting in the Dha residue which may be converted to any natural or unnatural amino acid residue desired without the alteration of the remainder of the peptide or protein. The invention also allows ligation of a desired peptide at any point rather than at a point where there should be a naturally occurring cysteine, thereby allowing native chemical ligation to be used in the synthesis of peptides that do not contain cysteine. The methodology allows for the synthesis of very large peptides.
本发明涉及一种将肽或蛋白质中的半胱
氨酸残基选择性转化为去氢丙
氨酸(Dha)残基的方法。该方法也适用于
硒半胱
氨酸和取代的半胱
氨酸和
硒半胱
氨酸残基,从而产生Dha残基,该残基可以转化为所需的任何天然或非天然
氨基酸残基,而不改变肽或蛋白质的其余部分。本发明还允许在任何点上连接所需的肽,而不是在应该存在天然半胱
氨酸的点上进行连接,从而允许在合成不含半胱
氨酸的肽时使用天然
化学连接。该方法允许合成非常大的肽。