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.
本研究提供了一种选择性修饰蛋白质或肽的 C-末端的简单而低成本的方法。修饰蛋白质或肽的 C 端的方法包括在需要进行 C 端修饰的蛋白质或肽的 C 端形成分子内
恶唑酮环,然后对
恶唑酮环进行开环反应,生成具有修饰 C 端的蛋白质或肽。优选的形式包括这样一种方法:通过使
噁唑酮环与含有亲核基团的化合物反应以实现
噁唑酮环开环,从而制备出一种蛋白质或肽,其中的 C-末端被含有亲核基团的化合物修饰、以及一种方法,在该方法中,通过使
噁唑酮环与活性酯化剂反应以实现开环,
噁唑酮被转化为活性酯,通过随后与含有亲核基团的化合物反应,产生一种蛋白质或肽,在该蛋白质或肽中,C-末端被含有亲核基团的化合物修饰。