Abstract: A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with 99mTc by a ligand exchange reaction. Like the 1st generation 99mTc-HYNIC-annexin A5, the novel 99mTc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat models of hepatic apoptosis there was 283% increase in hepatic uptake of 99mTc-cys-annexin A5 as compared to normal mice. The results indicate that the novel 99mTc-cys-annexin A5 is a potential apoptosis imaging agent.
Keywords: cys-annexin A5; 99mTc-labelled; biodistribution; apoptosis imaging
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Lu, C.; Jiang, Q.; Hu, M.; Tan, C.; Ji, Y.; Yu, H.; Hua, Z. Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent. Molecules 2013, 18, 6908-6918.
Lu C, Jiang Q, Hu M, Tan C, Ji Y, Yu H, Hua Z. Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent. Molecules. 2013; 18(6):6908-6918.
Lu, Chunxiong; Jiang, Quanfu; Hu, Minjin; Tan, Cheng; Ji, Yu; Yu, Huixin; Hua, Zichun. 2013. "Preliminary Biological Evaluation of Novel 99mTc-Cys-Annexin A5 as a Apoptosis Imaging Agent." Molecules 18, no. 6: 6908-6918.