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过去四年中,氟尿嘧啶的生物化学和药物动力学有了较大的进展。其中多数进展是技术革新的结果。最重要的是用高压液相色谱法测定5-氟尿嘧啶(FUra)及其代谢物的进展。第二个进展则是应用蛋白结合技术研究胸苷酸合成酶和5-氟脱氧尿嘧啶核苷一磷酸(FdUMP)间的相互作用。这不仅清楚地显示了抑制剂-酶相互作用的细节,而且还提供了测定FdUMP和胸苷酸合成酶的超常敏感的方法。本综述的目的是概括综合这些进展。一、5-氟尿嘧啶的代谢绝大多数证据表明,除活化的代谢物外,FUra对哺乳类细胞基本无害。代谢活化和代谢分解间平衡的详细知识对讨论其生化效
In the past four years, there has been a great deal of progress in the biochemistry and pharmacokinetics of fluorouracil. Most of these advances are the result of technological innovations. Most important is the determination of the progress of 5-fluorouracil (FUra) and its metabolites by high pressure liquid chromatography. The second progress is the application of protein binding technology to study the interaction between thymidylate synthase and 5-fluorodeoxyuridine nucleoside monophosphate (FdUMP). This not only shows clearly the details of inhibitor-enzyme interactions but also provides an extremely sensitive method of determining FdUMP and thymidylate synthase. The purpose of this review is to summarize these advances. First, the metabolism of 5 - fluorouracil The vast majority of evidence that, in addition to the activation of metabolites, FUra basically harmless to mammalian cells. Metabolic activation and metabolic balance between the detailed knowledge on the discussion of its biochemical effects