Site-specific 68Ga-labeled Annexin A5 as a PET imaging agent for apoptosis
Site-specific 68Ga-labeled Annexin A5 as a PET imaging agent for apoptosis
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DOI：
10.1016/j.nucmedbio.2010.09.008
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发表时间：
2011-04-01
影响因子：
3.1
通讯作者：
Verbruggen, Alfons
中科院分区：
文献类型：
--
作者：
Bauwens, Matthias;De Saint-Hubert, Marijke;Verbruggen, Alfons
目的：用 Gallium-68 标记膜联蛋白 A5 的两种变体（Cys2-AnxA5 和 Cys 165-AnxA5），以评估其生物学特性。 程序：使用 mu PET 在健康小鼠和肝细胞凋亡小鼠模型中研究放射性示踪剂的生物分布和药代动力学。在化疗和放疗联合治疗前后，对 Daudi 荷瘤小鼠进行 IV 注射示踪剂后结合 mu MRI 进行 mu PET 成像。结果：生物分布数据表明，尽管在肾脏中观察到较高的滞留，但尿清除率很快，肝胆清除率很小。与健康动物相比，接受抗 Fas 治疗的动物的肝脏摄取量高出 3 至 8 倍。肿瘤对Ga-68-Cys2-AnxA5和Ga-68-Cys165-AnxA5的摄取较低，但治疗后显着增加。结论：Ga-68-Cys2-AnxA5和Ga-65-Cys165-AnxA5均显示出与凋亡细胞的明显结合，是用于快速评估癌症治疗的有前景的示踪剂。 (C) 2011 Elsevier Inc. 保留所有权利。
Purpose: Two variants of Annexin A5 (Cys2-AnxA5 and Cys 165-AnxA5) were labelled with Gallium-68 in order to evaluate their biological properties.Procedures: Biodistribution and pharmacokinetics of the radiotracers were studied with mu PET in healthy mice and in a mouse model of hepatic apoptosis. mu PET imaging after IV injection of the tracers in combination with mu MRI was performed in Daudi tumor bearing mice before and after treatment with a combination of chemotherapy and radiotherapy.Results: The biodistribution data indicated a fast urinary clearance with only minor hepatobilliary clearance, although a high retention in the kidneys was observed. Animals treated with anti-Fas showed a 3 to 8 times higher liver uptake as compared to healthy animals. Tumor uptake of Ga-68-Cys2-AnxA5 and Ga-68-Cys165-AnxA5 was low but significantly increased after therapy.Conclusion: Both Ga-68-Cys2-AnxA5 and Ga-65-Cys165-AnxA5 show a clear binding to apoptotic cells and are promising tracers for rapid evaluation of cancer therapy. (C) 2011 Elsevier Inc. All rights reserved.