[en] Oligonucleotides (ONs) and more particularly siRNAs are promising drugs but their pharmacokinetics and biodistribution are widely unknown. Positron Emission Tomography (PET) using fluorine-18 is a suitable technique to quantify these biological processes. Click chemistry (Huisgen cycloaddition) is the current method for labeling siRNA. In order to study the influence of a linker bearing by [18F]labeled ONs, on the in vivo pharmacokinetic and metabolism, we have developed two modified ONs by two news linkers. Here we report the synthesis of two alkyne-bearing linkers, the incorporation onto a ONs and the conjugation by click chemistry with a [18F]prosthetic group.
Research Center/Unit :
GIGA CRC (Cyclotron Research Center) In vivo Imaging-Aging & Memory - ULiège
Disciplines :
Chemistry
Author, co-author :
Flagothier, Jessica ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse
Kaisin, Geoffroy ; Université de Liège - ULiège > Centre de recherches du cyclotron
Mercier, Frederic
Thonon, David ; Université de Liège - ULiège > Centre de recherches du cyclotron
Teller, Nathalie
Wouters, Johan
Luxen, André ; Université de Liège - ULiège > Département de chimie (sciences) > Chimie organique de synthèse
Language :
English
Title :
Synthesis of two new alkyne-bearing liners used for the preparation of siRNA for labeling by click chemistry with fluorine-18
Alternative titles :
[fr] Synthèse de deux linkers, porteurs d'un groupe alcyne, utilisés pour la preparation de siRNA pour le marquage au fluor-18 par chimie click.
