General method to label antisense oligonucleotides with radioactive halogens for pharmacological and imaging studies

被引：71

作者：

Kühnast, B ^{[1
]}

Dollé, F ^{[1
]}

Terrazzino, S ^{[1
]}

Rousseau, B ^{[1
]}

Loc'h, C ^{[1
]}

Vaufrey, F ^{[1
]}

Hinnen, F ^{[1
]}

Doignon, I ^{[1
]}

Pillon, F ^{[1
]}

David, C ^{[1
]}

Crouzel, C ^{[1
]}

Tavitian, B ^{[1
]}

机构：

[1] CEA, SHFJ, INSERM U334,DSV, Serv Mol Marquees, F-91401 Orsay, France

来源：

BIOCONJUGATE CHEMISTRY | 2000年 / 11卷 / 05期

关键词：

D O I：

10.1021/bc990183i

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Evaluation of oligonucleotides for biomedical applications requires different in vivo and in vitro approaches (pharmacokinetics, biodistribution, macro- and microimaging, metabolism,...), that are performed with different radioisotopes according to the temporal and spatial resolution needed. A method to introduce radioactive isotopes of halogens (fluorine, bromine, and iodine) in a small and stable molecule has been developed. Radiosynthons can then be conjugated with any given oligonucleotide in one step to create the appropriate radiotracer. This general radiolabeling procedure for oligonucleotides is efficient to synthesize F-18-, Br-76-, and I-125-oligonucleotides for biological needs. Applications of the method to biodistribution, metabolism, in vivo and ex vivo imaging of I-125- and F-18-labeled oligonucleotides are reported.

引用

页码：627 / 636

页数：10

共 46 条

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