Abuchowski A, van Es T, Palczuk N C, McCoy J R, Davis F F
Cancer Treat Rep. 1979 Jun;63(6):1127-32.
An L-glutaminase-L-asparaginase from Achromobacter has been rendered nonimmunogenic by the covalent attachment of polyethylene glycol (PEG) to nonessential amine groups of the enzyme. PEG-L-glutaminase-L-asparaginase exhibits a greatly enhanced half-life in the bloodstream compared to the unmodified enzyme in normal mice, and is effective in prolonging the survival of BDF1 mice inoculated ip with L5178Y cells. PEG-L-glutaminase-L-asparaginase appears rapidly in the blood following ip injection.
通过将聚乙二醇(PEG)共价连接到无色杆菌的L-谷氨酰胺酶-L-天冬酰胺酶的非必需胺基上,使其失去免疫原性。与正常小鼠体内未修饰的酶相比,聚乙二醇化L-谷氨酰胺酶-L-天冬酰胺酶在血液中的半衰期大大延长,并且在延长腹腔接种L5178Y细胞的BDF1小鼠的存活时间方面有效。腹腔注射后,聚乙二醇化L-谷氨酰胺酶-L-天冬酰胺酶迅速出现在血液中。