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[重氮丝氨酸和6-重氮-5-氧代-L-正亮氨酸对微生物谷氨酰胺(天冬酰胺)酶的灭活作用]

[Inactivation of microbial glutamin-(asparagin-)ase by azaserine and 6-diazo-5-oxo-L-norleucine].

作者信息

Lebedeva Z I, Kabanova E A, Berezov T T

出版信息

Biull Eksp Biol Med. 1985 Dec;100(12):696-8.

PMID:4074870
Abstract

The effect of substrate analogues on glutamin-(asparagin-)ase from Pseudomonas aurantiaca-548 has been studied. The enzyme was demonstrated to be highly sensitive to the the action of 6-diazo-5-oxo-L-norleucine and azaserine. L-isomers of glutamine, aspartate, glutamate and several other substrate analogues with free alpha-amino groups protected the enzyme against the inhibitory DON effect. Thus, thorough preliminary selection of appropriate inhibitors, their dosage and treatment duration is needed for the recommendation of combined enzyme-inhibitor application in anti-tumour chemotherapy.

摘要

研究了底物类似物对橙色假单胞菌-548谷氨酰胺酶(天冬酰胺酶)的影响。已证明该酶对6-重氮-5-氧代-L-正亮氨酸和重氮丝氨酸的作用高度敏感。谷氨酰胺、天冬氨酸、谷氨酸的L-异构体以及其他几种带有游离α-氨基的底物类似物可保护该酶免受抑制性DON效应的影响。因此,在推荐联合酶抑制剂应用于抗肿瘤化疗时,需要对合适的抑制剂、其剂量和治疗持续时间进行全面的初步筛选。

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