Fluorine-18 labelling of small interfering RNAs (siRNAs) for PET imaging

被引：25

作者：

Viel, Thomas ^{[1
,2
]}

Kuhnast, Bertrand ^{[1
]}

Hinnen, Francoise ^{[1
]}

Boisgard, Raphael ^{[1
,2
]}

Tavitian, Bertrand ^{[1
,2
]}

Dolle, Frederic ^{[1
]}

机构：

[1] CEA, Serv Hosp Frederic Joliot, Inst Imagerie Biomed, DSV,I2BM,SHFJ,LIME,Lab Imagerie Mol Expt, F-91401 Orsay, France

[2] CEA, Serv Hosp Frederic Joliot, Lab Imagerie Express Genes, DSV,I2BM,SHFJ,LIEG INSERM U 803,Inst Imag Biomed, F-91401 Orsay, France

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2007年 / 50卷 / 13-14期

关键词：

fluorine-18; siRNA; oligonucleotide; FPyBrA;

D O I：

10.1002/jlcr.1411

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Small interfering RNAs (siRNAs), a class of macromolecules constituted by the association of two single-stranded ribonucleic acids of short sequences, have been labelled with the positron-emitter fluorine-18 (T-1/2: 109.8 min). The strategy involves (1) prosthetic conjugation of a single-stranded oligonucleotide with [F-18]FPyBrA (N-[3-(2-[F-18]fluoropyridin-3-yloxy)-propyl]-2-bromoacetamide) followed by (2) formation of the target duplex by annealing with the complementary sequence, therefore, permitting parallel and combinatorial preparation of [F-18]siRNAs. Pure fluorine-18-labelled siRNAs (0.55-1.11 GBq, specific activity: 74-148 GBq/mu mol at EOB) could be obtained within 165 min starting from 37.0 GBq of starting [F-18]fluoride (1.5-3.0%, non-decay-corrected isolated yields). Copyright (C) 2007 John Wiley & Sons, Ltd.

引用

页码：1159 / 1168

页数：10