化学修饰解除天冬酰胺酶抗原性研究

Chemical Modification of L-Asparaginase to Eliminate Its Antideniclty

本文报道了用活化的单甲氧基聚乙二醇PEG_2在底物保护的条件下修饰天冬酰胺酶。结果,修饰酶在抗原抗体结合能力完全消失的同时,酶活力保持30％以上,且修饰酶的抗胰蛋白酶水解能力明显增强,体外半衰期延长17倍,免疫原性显著下降。

The L-asparaginase was modified with activated PEG2[2.4-bis(o-mono-methoxypolyethlene glycol of 5000 daltons)-g-chloro-s-triazine], its antigenicity being removed completely, possessed activity over 30 per cent of native enzyme. The enzyme having 51 of all 92 free amino groups modified. The immunogenicity of modified enzyme was greatly decreased. The properties of enzymes, such as halt life (in vitro) and resistant ability to proteolysis was reported.