Inaba M
Cancer Chemotherapy Center, Japanese Foundation for Cancer Research.
Gan To Kagaku Ryoho. 1988 Mar;15(3):380-91.
About 30 kinds of biochemical modulators of 5-fluorouracil (5-FU) are described. They modify the metabolism and cytotoxic action of 5-FU through an alteration in (1) intracellular concentration of 5-FU or its metabolites, (2) intracellular pool of co-substrates essential for 5-FU metabolism, and (3) intracellular pool of normal substrates which compete with 5-FU metabolism. As a result, they affect either its inhibitory effect on thymidylate synthase or incorporation into RNA, or both. Thus, some of these modulators can improve antitumor activity of 5-FU by potentiating its tumor-selective toxicity or reducing its host toxicity selectively. From such various points of view, a variety of biochemical modulators of 5-FU are reviewed.
本文描述了约30种5-氟尿嘧啶（5-FU）的生化调节剂。它们通过改变以下方面来调节5-FU的代谢和细胞毒性作用：（1）5-FU或其代谢产物的细胞内浓度；（2）5-FU代谢所必需的共底物的细胞内库；（3）与5-FU代谢竞争的正常底物的细胞内库。结果，它们要么影响其对胸苷酸合成酶的抑制作用，要么影响其掺入RNA，或者两者都有影响。因此，其中一些调节剂可以通过增强其肿瘤选择性毒性或选择性降低其宿主毒性来提高5-FU的抗肿瘤活性。从这些不同的角度，对5-FU的各种生化调节剂进行了综述。
