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

共 51 条

[41] Positional effect of chemical modifications on short interference RNA activity in mammalian cells [J].

Prakash, TP ;

Allerson, CR ;

Dande, P ;

Vickers, TA ;

Sioufi, N ;

Jarres, R ;

Baker, BF ;

Swayze, EE ;

Griffey, RH ;

Bhat, B .

JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (13) :4247-4253

[42] Sensing the danger in RNA [J].

Robbins, MA ;

Rossi, JJ .

NATURE MEDICINE, 2005, 11 (03) :250-251

[43] Activation of the interferon system by short-interfering RNAs [J].

Sledz, CA ;

Holko, M ;

de Veer, MJ ;

Silverman, RH ;

Williams, BRG .

NATURE CELL BIOLOGY, 2003, 5 (09) :834-839

[44] siRNA and miRNA: an insight into RISCs [J].

Tang, GL .

TRENDS IN BIOCHEMICAL SCIENCES, 2005, 30 (02) :106-114

[45] In vivo imaging of oligonucleotides with positron emission tomography [J].

Tavitian, B ;

Terrazzino, S ;

Kühnast, B ;

Marzabal, S ;

Stettler, O ;

Dollé, F ;

Deverre, JB ;

Jobert, A ;

Hinnen, F ;

Bendriem, B ;

Crouzel, C ;

Di Giamberardino, L .

NATURE MEDICINE, 1998, 4 (04) :467-471

[46]

Tavitian B, 2003, GUT, V52, P40

[47] Characterization of a synthetic anionic vector for oligonucleotide delivery using in vivo whole body dynamic imaging [J].

Tavitian, B ;

Marzabal, S ;

Boutet, V ;

Kühnast, B ;

Terrazzino, S ;

Moynier, M ;

Dollé, F ;

Deverre, JR ;

Thierry, AR .

PHARMACEUTICAL RESEARCH, 2002, 19 (04) :367-376

[48] The genetics of RNA silencing [J].

Tijsterman, M ;

Ketting, RF ;

Plasterk, RHA .

ANNUAL REVIEW OF GENETICS, 2002, 36 :489-519

[49]

VIEL T, UNPUB

[50] RADIOHALOGENATION OF PROTEINS - AN OVERVIEW OF RADIONUCLIDES, LABELING METHODS, AND REAGENTS FOR CONJUGATE LABELING [J].

WILBUR, DS .

BIOCONJUGATE CHEMISTRY, 1992, 3 (06) :433-470

← 1 2 3 4 5 6 →