Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18

Jessica Flagothier; Geoffroy Kaisin; Frederic Mercier; David Thonon; Nathalie Teller; Johan Wouters; André Luxen

doi:10.1016/j.apradiso.2012.04.022

Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18

Jessica Flagothier, Geoffroy Kaisin, Frederic Mercier, David Thonon, Nathalie Teller, Johan Wouters, André Luxen

Universite de Namur

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

Résumé

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.

langue originale	Anglais
Pages (de - à)	1549-1557
Nombre de pages	9
journal	Applied Radiation and Isotopes
Volume	70
Numéro de publication	8
Les DOIs	https://doi.org/10.1016/j.apradiso.2012.04.022
Etat de la publication	Publié - 1 août 2012

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10.1016/j.apradiso.2012.04.022

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@article{77593f1a7c144444a437bc8175bc63a1,

title = "Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18",

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.",

keywords = "Click chemistry, Fluorine-18, PET, Radiochemistry, SiRNA",

author = "Jessica Flagothier and Geoffroy Kaisin and Frederic Mercier and David Thonon and Nathalie Teller and Johan Wouters and Andr{\'e} Luxen",

year = "2012",

month = aug,

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doi = "10.1016/j.apradiso.2012.04.022",

language = "English",

volume = "70",

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journal = "Applied Radiation and Isotopes",

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Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18. / Flagothier, Jessica; Kaisin, Geoffroy; Mercier, Frederic et al.
Dans: Applied Radiation and Isotopes, Vol 70, Numéro 8, 01.08.2012, p. 1549-1557.

Résultats de recherche: Contribution à un journal/une revue › Article › Revue par des pairs

TY - JOUR

T1 - Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18

AU - Flagothier, Jessica

AU - Kaisin, Geoffroy

AU - Mercier, Frederic

AU - Thonon, David

AU - Teller, Nathalie

AU - Wouters, Johan

AU - Luxen, André

PY - 2012/8/1

Y1 - 2012/8/1

N2 - 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.

AB - 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.

KW - Click chemistry

KW - Fluorine-18

KW - PET

KW - Radiochemistry

KW - SiRNA

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U2 - 10.1016/j.apradiso.2012.04.022

DO - 10.1016/j.apradiso.2012.04.022

M3 - Article

C2 - 22732389

AN - SCOPUS:84862629483

SN - 0969-8043

VL - 70

SP - 1549

EP - 1557

JO - Applied Radiation and Isotopes

JF - Applied Radiation and Isotopes

IS - 8

ER -

Synthesis of two new alkyne-bearing linkers used for the preparation of siRNA for labeling by click chemistry with fluorine-18

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