对2'-脱氧-2'-[(18)F]氟-5-碘-1-β-D-阿拉伯呋喃糖基尿嘧啶（[18F]FIAU）和2'-脱氧-2'-[18F]氟-5-乙基-1-β-D-阿拉伯呋喃糖基尿嘧啶（[18F]FEAU）作为自杀基因表达标志物的体内评估。
In vivo evaluation of 2'-deoxy-2'-[(18)F]fluoro-5-iodo-1-beta-D-arabinofuranosyluracil ([18F]FIAU) and 2'-deoxy-2'-[18F]fluoro-5-ethyl-1-beta-D-arabinofuranosyluracil ([18F]FEAU) as markers for suicide gene expression.
作者信息
Alauddin Mian M, Shahinian Antranic, Park Ryan, Tohme Michel, Fissekis John D, Conti Peter S
机构信息
University of Texas MD Anderson Cancer Center, 1515 Holcombe Blvd. T8.3895, P.O. Box 059, Houston, TX 77030, USA.
出版信息
Eur J Nucl Med Mol Imaging. 2007 Jun;34(6):822-9. doi: 10.1007/s00259-006-0305-1. Epub 2007 Jan 6.
PURPOSE
FIAU and FEAU were evaluated in vitro and in vivo as markers for HSV1-tk gene expression.
METHODS
In vitro and biodistribution studies were performed in wild type and transduced HT-29 cells using [14C]FIAU and [3H]FEAU. PET imaging was performed using [18F]FIAU and [18F]FEAU.
RESULTS
In vitro uptake of [14C]FIAU in tk-positive cells was 39-fold, 49-fold, and 43-fold higher (p<0.001) than in wild type cells at 30, 60, and 120 min, respectively. Uptake of [3H]FEAU in transduced cells was 46-fold, 62-fold, and 121-fold higher (p<0.001) than in wild type cells at the same time points. In vivo uptake of [14C]FIAU at 2 h in HSV1-tk positive tumors was 15.48+/-3.94, 6.7-fold higher (p<0.001) than in wild type tumors. Uptake of [3H]FEAU in transduced tumors was 9.98+/-1.99, 5.0-fold higher (p<0.001) than in wild type tumors. Micro-PET images using [18F]FIAU and [18F]FEAU also showed very high uptake in HSV-tk tumors.
CONCLUSION
[18F]FIAU and [18F]FEAU appear to be potential PET imaging agents for gene expression.
目的
在体外和体内评估FIAU和FEAU作为单纯疱疹病毒1型胸苷激酶（HSV1-tk）基因表达标志物的情况。
方法
使用[14C]FIAU和[3H]FEAU在野生型和转导的HT-29细胞中进行体外和生物分布研究。使用[18F]FIAU和[18F]FEAU进行正电子发射断层扫描（PET）成像。
结果
在30、60和120分钟时，tk阳性细胞中[14C]FIAU的体外摄取量分别比野生型细胞高39倍、49倍和43倍（p<0.001）。在相同时间点，转导细胞中[3H]FEAU的摄取量比野生型细胞高46倍、62倍和121倍（p<0.001）。HSV1-tk阳性肿瘤在2小时时[14C]FIAU的体内摄取量为15.48±3.94，比野生型肿瘤高6.7倍（p<0.001）。转导肿瘤中[3H]FEAU的摄取量为9.98±1.99，比野生型肿瘤高5.0倍（p<0.001）。使用[18F]FIAU和[18F]FEAU的微型PET图像也显示HSV-tk肿瘤摄取量非常高。
结论
[18F]FIAU和[18F]FEAU似乎是用于基因表达的潜在PET成像剂。
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