Site-specific labeling of 'second generation' annexin V with 99mTc(CO)3 for improved imaging of apoptosis in vivo

Site-specific labeling of 'second generation' annexin V with 99mTc(CO)3 for improved imaging of apoptosis in vivo
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DOI:
10.1016/j.bmc.2009.12.021
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发表时间:
2010-02-01
影响因子:
3.5
通讯作者:
Rattat, Dirk
Rattat, Dirk
中科院分区:
医学3区
文献类型:
--
作者:
De Saint-Hubert, Marijke;Mottaghy, Felix M.;Rattat, Dirk

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在这项研究中,“第二代”AnxV 在蛋白质结合区域之外以三种不同的方式用 Tc-99m 进行特异性标记,以获得改进的靶点与背景活性比。这些化合物在正常小鼠和肝细胞凋亡模型(抗 Fas mAb)中进行了体外和体内测试。与 Tc-99m-HYNIC-cys-AnxV 和 Tc-99m(CO)(3)-DTPA-cys-AnxV 相比,用 Tc-99m(CO)(3) 标记的 HIS 标记“第二代”AnxV 的凋亡结合最为显着。 (C) 2009 Elsevier Ltd. 保留所有权利。
In this study 'second generation' AnxV was specifically labeled with Tc-99m in three different ways outside the binding region of the protein to obtain an improved target-to-background activity ratio. The compounds were tested in vitro and in vivo in normal mice and in a model of hepatic apoptosis (anti-Fas mAb). The apoptosis binding was most prominent for the HIS-tagged 'second generation' AnxV labeled with Tc-99m(CO)(3) in comparison to Tc-99m-HYNIC-cys-AnxV and Tc-99m(CO)(3)-DTPA-cys-AnxV. (C) 2009 Elsevier Ltd. All rights reserved.