用¹⁸⁸Re以高标记效率和比活度对MAG3吗啉代寡聚物进行放射性标记用于肿瘤预靶向。
Radiolabeling of MAG3-morpholino oligomers with 188Re at high labeling efficiency and specific radioactivity for tumor pretargeting.
作者信息
Liu Guozheng, Dou Shuping, He Jiang, Yin Dongguang, Gupta Suresh, Zhang Surong, Wang Yi, Rusckowski Mary, Hnatowich Donald J
机构信息
Division of Nuclear Medicine, Department of Radiology, University of Massachusetts Medical School, 55 Lake Avenue North, Worcester, MA 01655, USA.
出版信息
Appl Radiat Isot. 2006 Sep;64(9):971-8. doi: 10.1016/j.apradiso.2006.04.005. Epub 2006 May 30.
Abstract
We are investigating a novel pretargeting approach involving an initial IV injection of antitumor antibody conjugated with a phosphorodiamidate morpholino oligomer (MORF, a DNA analog) and the subsequent IV injection of the radiolabeled complement oligomer (cMORF). In this paper, the cMORF was labeled with (188)Re using MAG(3) as chelator for therapeutic applications. Since (c)MORFs are unstable in acidic condition, an optimal labeling pH was first selected and the other labeling factors were then examined. A labeling efficiency of greater than 90% can be achieved even at a concentration of MAG(3)-cMORF as low as 0.8 microM. The labeled cMORF is stable and capable of hybridizing to its complement.
摘要
我们正在研究一种新型预靶向方法，该方法包括首次静脉注射与磷酰胺吗啉代寡聚物（MORF，一种DNA类似物）偶联的抗肿瘤抗体，随后静脉注射放射性标记的互补寡聚物（cMORF）。在本文中，cMORF用（188）Re标记，使用MAG(3)作为螯合剂用于治疗应用。由于（c）MORF在酸性条件下不稳定，首先选择了最佳标记pH，然后检查了其他标记因素。即使在MAG(3)-cMORF浓度低至0.8 microM的情况下，标记效率也能达到90%以上。标记的cMORF是稳定的，能够与其互补物杂交。
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