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11. 发明申请

US20050085622A1 Method for modifying protein or peptide C-terminal 有权
标题翻译：蛋白质或肽C端修饰方法
公开(公告)号：US20050085622A1
公开(公告)日：2005-04-21
申请号：US10958298
申请日：2004-10-06
申请人： Takashi Nakazawa , Minoru Yamaguchi , Hiroki Kuyama , Eiji Ando , Norikazu Ueyama , Taka-aki Okamura , Shigemi Norioka
发明人： Takashi Nakazawa , Minoru Yamaguchi , Hiroki Kuyama , Eiji Ando , Norikazu Ueyama , Taka-aki Okamura , Shigemi Norioka
IPC分类号： C07K1/113 , C07K1/00 , C07K1/08 , C07K14/00
CPC分类号： C07K1/003
摘要： A simple and low-cost method of selectively modifying the C-terminal of a protein or peptide is provided. A method of modifying the C-terminal of a protein or peptide comprises forming an intramolecular oxazolone ring at the C-terminal of the protein or peptide that requires C-terminal modification, and then performing a ring-opening of the oxazolone ring to produce a protein or peptide with a modified C-terminal. Preferred forms include a method in which by reacting the oxazolone ring with a compound containing a nucleophilic group to effect an oxazolone ring-opening, a protein or peptide is produced in which the C-terminal is modified with the compound containing the nucleophilic group, as well as a method in which by reacting the oxazolone ring with an active esterifying agent to effect a ring-opening, the oxazolone is converted to an active ester, which by subsequent reaction with a compound containing a nucleophilic group, produces a protein or peptide in which the C-terminal has been modified with the compound containing the nucleophilic group.
摘要翻译：提供了选择性修饰蛋白质或肽的C-末端的简单且低成本的方法。修饰蛋白质或肽的C末端的方法包括在需要C末端修饰的蛋白质或肽的C-末端形成分子内的恶唑酮环，然后进行恶唑酮环的开环以产生具有修饰C末端的蛋白质或肽。优选的形式包括通过使恶唑酮环与含有亲核基团的化合物反应以进行恶唑酮开环的方法，制备其中C-末端用含有亲核基团的化合物修饰的蛋白质或肽作为以及通过使恶唑酮环与活性酯化剂反应以开环的方法，将恶唑酮转化成活性酯，其随后与含有亲核基团的化合物反应，产生蛋白质或肽其中C-末端已经与含有亲核基团的化合物一起被修饰。

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