肿瘤增殖显像剂3'-脱氧-3'-18F-氟代胸苷

18F-氟代脱氧葡萄糖(18F-FDG)是广泛用于肿瘤诊断的PET显像剂,由于所有细胞都利用葡萄糖,因此,18F-FDG不是特异的肿瘤显像剂.3'-脱氧-3'-18F-氟代胸苷(18F-FLT)克服了18F-FDG的局限性,并可以进行细胞增殖显像.对于肿瘤的PET研究,18F-FLT是理想的反映增殖特性的示踪剂,18F-FLT利用胸苷激酶催化的磷酸化作用来评价DNA复制过程,可以准确地评估肿瘤细胞DNA的合成和细胞增殖活性,可用于肿瘤的早期诊断及鉴别诊断、化疗和放疗的疗效监测,是很有希望和发展前途的PET显像剂.

The current status of 18F-FLT as a proliferation tracer

~(18)F-fluorodeoxyglucose (~(18)F-FDG) is widely used to detect tumor with PET. However, 18F-FDG is not specific for tumor imaging because glucose is also utilized by other benign cells. 3'-deoxy-3'-18F-fluorothymi-dine (18F-FLT) is developed to overcome the limitations of 18F-FDG and to image cellular proliferation by PET. 18F-FLT features an excellent proliferation tracer for PET studies of tumors. The advantage of 18F-FLT is based on thymidine kinase-1(TK1) catalyzed phosphorylation of FLT and the intracellular accumulation of 18F-FLT is dependent on the presence of TK1, which is closely related to cellular proliferation in tumor cells undergoing DNA replication during the S phase of the cell cycle. Therefore, 18F-FLT is expected to be a feasible PET tracer for diagnosing, evaluating and monitoring the early response to therapy in oncology.