Preparation, in vitro and in vivo evaluation of 99mTc-Annexin B1: A novel radioligand for apoptosis imaging

To develop a radiopharmaceutical for apoptosis imaging, Annexin B1, a new Ca 2+-dependent phosphatidylserine (PS)-binding protein, was directly radiolabeled with 99mTc. This procedure yields up to 96% of radiochemical purity and higher radiolabeling efficiency. The preparation has been found to be s...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 2005-10, Vol.335 (4), p.1102-1106
Main Authors: Luo, Quan-yong, Zhang, Zhi-yong, Wang, Fang, Lu, Han-kui, Guo, Yu-zhi, Zhu, Rui-sen
Format: Article
Language:English
Subjects:
99mTc
Annexin B1
Apoptosis
Radionuclide imaging
Radiopharmaceutical
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Summary:To develop a radiopharmaceutical for apoptosis imaging, Annexin B1, a new Ca 2+-dependent phosphatidylserine (PS)-binding protein, was directly radiolabeled with 99mTc. This procedure yields up to 96% of radiochemical purity and higher radiolabeling efficiency. The preparation has been found to be sufficiently stable in vitro. Binding assay with human activated platelets indicated that 99mTc-Annexin B1 retained its PS binding activity. Biodistribution in mice revealed that 99mTc-Annexin B1 rapidly cleared from the blood and predominantly accumulated in the kidney. The increase in hepatic uptake in anti-Fas antibody treated mice correlated to histologic evidence of fulminant hepatic apoptosis. These data suggest that 99mTc-Annexin B1 can be used as a novel radiotracer to detect apoptosis in vivo.
ISSN:0006-291X
1090-2104
DOI:10.1016/j.bbrc.2005.07.188