Ornithine decarboxylase in Trypanosoma brucei brucei: evidence for selective toxicity of difluoromethylornithine.
Ornithine decarboxylase in Trypanosoma brucei brucei: evidence for selective toxicity of difluoromethylornithine.
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布氏锥虫中的鸟氨酸脱羧酶：二氟甲基鸟氨酸选择性毒性的证据。
DOI：
10.1111/j.1550-7408.1982.tb05418.x
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发表时间：
1982
期刊：
影响因子：
--
通讯作者：
Hutner,SH
中科院分区：
文献类型：
--
作者：
Garofalo,J;Bacchi,CJ;McLaughlin,SD;Mockenhaupt,D;Trueba,G;Hutner,SH
鸟氨酸脱羧酶是多胺生物合成的主要限速酶，在布氏锥虫的血流中测定其活性。该酶需要 5′-磷酸吡哆醛、二硫苏糖醇和 EDTA 才能获得最佳活性。研究了该酶的一些特性并与哺乳动物酶进行了比较。最值得注意的是，寄生虫酶对抑制剂 DL-α-二氟甲基鸟氨酸的敏感性比哺乳动物对应物高 60 倍以上，从而使其成为有吸引力的化疗靶点。
Activity of ornithine decarboxylase, the major rate limiting enzyme of polyamine biosynthesis, was determined in bloodstream trypomastigotes ofTrypanosoma brucei brucei.The enzyme required pyridoxal‐5′‐phosphate, dithiothreitol and EDTA for optimal activity. Several properties of the enzyme were investigated and compared to the mammalian enzyme. Most notably, the parasite enzyme was >60‐fold more sensitive to the inhibitor DL‐α‐difluoromethylornithine than its mammalian counterpart, thus making it an attractive target for chemotherapy.