Development of labeled thymidine analogs for imaging tumor proliferation
Development of labeled thymidine analogs for imaging tumor proliferation
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DOI：
10.1016/0969-8051(95)02005-5
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发表时间：
1996-01-01
影响因子：
3.1
通讯作者：
Zheng, M
中科院分区：
文献类型：
--
作者：
Shields, AF;Grierson, JR;Zheng, M
我们已经寻找了适合用F-18标记的核苷类似物，其可以用于用正电子发射断层扫描（PET）对肿瘤增殖进行成像。用氚标记以下三种胸苷类似物，并对其在小鼠体内的分解代谢和生物分布进行筛选：5-氟-1-（2 '-脱氧-2'-氟-β-D-呋喃核糖基）尿嘧啶（FFUdR）、5-氟-1-（2 '-脱氧-2'-氟-β-D-阿拉伯呋喃糖基）尿嘧啶（FFaraU）和5-甲基-1-（2 '-脱氧-2'-氟-β-D-呋喃核糖基）尿嘧啶（FTdR）。我们发现，所有三种化合物在体内和在血液中孵育时降解稳定。在所测试的三种类似物中，只有FFUdR在快速增殖的组织（例如脾和植入的肿瘤）中表现出优先保留，并且其在2小时时达到2.1的组织与血液比率。
We have sought nucleoside analogs suitable for labeling with F-18 that could be used to image tumor proliferation with positron emission tomography (PET). The following three thymidine analogs were labeled with tritium and screened for their catabolism and biodistribution in vivo in mice: 5-fluoro-1-(2 '-deoxy-2 '-fluoro-beta-D-ribofuranosyl)uracil (FFUdR), 5-fluoro-1-(2 '-deoxy-2 '-fluoro-beta-D-arabinofuranosyl)uracil (FFaraU) and 5-methyl-1-(2 '-deoxy-2 '-fluoro-beta-D-ribofuranosyl)uracil (FTdR). We found that all three compounds were stable to degradation in vivo and when incubated in blood. Of the three analogs tested, only FFUdR showed preferential retention in rapidly proliferating tissues, such as the spleen and implanted tumors, and it attained tissue to blood ratios of 2.1 at 2 h.