5-氟尿嘧啶(5-FU)自1957年问世以来,已被广泛应用于胃肠、头、颈、胸和卵巢等部位恶性肿瘤的治疗。作为嘧啶类似物,5-FU通过抑制胸苷酸合成酶并将其代谢产物整合到DNA和RNA中发挥抗癌作用。5-FU单药或联合用药虽至今仍用于胃肠道恶性肿瘤的一线治疗,但因患者易对其产生耐药性而使总体有效率降低。5-FU化疗耐药可能源自于酶的异常、基因异常和肿瘤微环境异常等因素。本文对5-FU作用机制及其化疗耐药机制的研究进展做一综述。
5-Fluorouracil(5-FU)has been widely used to treat gastrointestinal,head,neck,chest and ovarian malignant tumors since 1957. As an analogue of pyrimidine,5-FU plays anti-cancer roles by inhibiting thymioylate synthase and integrating its metabolites into DNA and RNA. Although 5-FU is one of the first-line therapeutic compounds for gastrointestinal malignant tumor as a single drug or in combination with other drugs,its effectiveness is hindered by its low efficiency,which may be due to chemotherapy resistance. 5-FU chemotherapy resistance may stem from enzyme abnormality,genetic abnormality and tumor microenvironment. In this paper,we make a review about 5-FU actions and the mechanisms underlying chemotherapy resistance.