Synthèse de deux linkers, porteurs d'un groupe alcyne, utilisés pour la preparation de siRNA pour le marquage au fluor-18 par chimie click.

  • Flagothier, Jessica
  • Kaisin, Geoffroy
  • Mercier, Frederic
  • Thonon, David
  • Teller, Nathalie
  • Wouters, Johan
  • Luxen, André
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Publication date
August 2012
Publisher
Pergamon Press

Abstract

peer reviewedOligonucleotides (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.OligoPE

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