Abstract
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 new 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.
Original language | English |
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Pages (from-to) | 1549-1557 |
Number of pages | 9 |
Journal | Applied Radiation and Isotopes |
Volume | 70 |
Issue number | 8 |
DOIs | |
Publication status | Published - 1 Aug 2012 |
Keywords
- Click chemistry
- Fluorine-18
- PET
- Radiochemistry
- SiRNA
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Physical Chemistry and characterization(PC2)
Johan Wouters (Manager) & Carmela Aprile (Manager)
Technological Platform Physical Chemistry and characterizationFacility/equipment: Technological Platform