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    • 12. 发明授权
    • Site specific protein modification
    • 位点特异性蛋白质修饰
    • US06433158B1
    • 2002-08-13
    • US09580235
    • 2000-05-26
    • Dean K. Pettit
    • Dean K. Pettit
    • C07K100
    • C07K1/1077A61K47/60A61K47/62C07K14/7151
    • Processes for conjugating proteins with polyethylene glycol are disclosed. The disclosed processes provide modified proteins having little or no decrease in their activity and include the steps of deleting at least one amino acid residue on the protein, replacing the at least one amino acid residue with an amino acid residue that does not react with, polyethylene glycol, and contacting the protein with polyethylene glycol under conditions sufficient to conjugate the polyethylene glycol to the protein. This advantageous retention of a desired protein activity is attributed to the availability of one or more protein binding sites which is unaltered in the conjugation process and thus remains free to interact with a binding partner ligand or cognate subsequent to the conjugation process.
    • 公开了将蛋白质与聚乙二醇缀合的方法。 所公开的方法提供了其活性几乎没有或没有降低的修饰的蛋白质,包括删除蛋白质上的至少一个氨基酸残基的步骤,用与聚乙烯不反应的氨基酸残基替换至少一个氨基酸残基 乙二醇,并且在足以使聚乙二醇与蛋白质缀合的条件下使蛋白质与聚乙二醇接触。 所需蛋白质活性的这种有利的保留归因于在缀合过程中未改变的一个或多个蛋白质结合位点的可用性,因此在缀合过程之后保持与结合配偶体配体或同源物相互作用。