用 99mTc(CO)3 对“第二代”膜联蛋白 V 进行位点特异性标记，以改善体内细胞凋亡的成像。

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

机构信息

Department of Nuclear Medicine, University Hospital Gasthuisberg Leuven, Herestraat 49, B-3000 Leuven, Belgium.

出版信息

Bioorg Med Chem. 2010 Feb;18(3):1356-63. doi: 10.1016/j.bmc.2009.12.021. Epub 2010 Jan 5.

DOI:10.1016/j.bmc.2009.12.021

PMID:20053567

Abstract

In this study 'second generation' AnxV was specifically labeled with (99m)Tc 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 (99m)Tc(CO)(3) in comparison to (99m)Tc-HYNIC-cys-AnxV and (99m)Tc(CO)(3)-DTPA-cys-AnxV.

摘要

在这项研究中，“第二代”AnxV 通过三种不同的方式在蛋白结合区域外进行了（99m）Tc 标记，以获得更好的靶标与背景的活性比。这些化合物在正常小鼠体内和肝凋亡模型（抗 Fas mAb）中进行了体外和体内测试。与（99m）Tc-HYNIC-cys-AnxV 和（99m）Tc(CO)(3)-DTPA-cys-AnxV 相比，标记有（99m）Tc(CO)(3)的 HIS 标记的“第二代”AnxV 的凋亡结合最为明显。