Higley B, Oakes J, De Mello J, Giles G R
Gut. 1982 Dec;23(12):1072-6. doi: 10.1136/gut.23.12.1072.
5-Fluorouracil (5-FU) requires activation to the metabolites FdUMP and FUTP for its cytotoxic effect. This activation involves the intracellular enzymes uridine and thymidine phosphorylase. We have assayed the levels of these enzymes in colorectal and gastric cancers and have shown that, in the majority of cases, the enzyme levels were higher than in the adjacent normal mucosa. It is suggested that, while the ratio tumour/normal mucosa enzyme activity may give some indication of the relative toxicity of 5-FU in these tissues, the absolute activities of the phosphorylases in tumour tissue could give a better indication of tumour responsiveness.
5-氟尿嘧啶(5-FU)需要被激活为代谢产物氟脱氧尿苷一磷酸(FdUMP)和氟尿嘧啶核苷三磷酸(FUTP)才能发挥其细胞毒性作用。这种激活过程涉及细胞内的尿苷磷酸化酶和胸苷磷酸化酶。我们检测了结直肠癌和胃癌中这些酶的水平,结果表明,在大多数病例中,这些酶的水平高于相邻的正常黏膜组织。有人提出,虽然肿瘤/正常黏膜组织的酶活性比值可能在一定程度上反映5-FU在这些组织中的相对毒性,但肿瘤组织中磷酸化酶的绝对活性可能更能体现肿瘤对5-FU的反应性。