ORBi: Kaisin Geoffroy - Click chemistry : radiolabelling of oligonucleotides with fluorine- 18 for PET

Reference : Click chemistry : radiolabelling of oligonucleotides with fluorine- 18 for PET


	Document type :	Scientific congresses and symposiums : Poster
	Discipline(s) :	Physical, chemical, mathematical & earth Sciences : Chemistry
	To cite this reference:	http://hdl.handle.net/2268/62864

Title :	Click chemistry : radiolabelling of oligonucleotides with fluorine- 18 for PET
Language :	English
Author, co-author :	Kaisin, Geoffroy [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Flagothier, Jessica [Université de Liège - ULg > Département de chimie (sciences) > Chimie organique de synthèse >]
	Mercier, Frédéric [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Thonon, David [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Paris, Jérôme [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Kech, Cécile [ > > ]
	Lemaire, Christian [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Plenevaux, Alain [Université de Liège - ULg > > Centre de recherches du cyclotron >]
	Luxen, André [Université de Liège - ULg > Département de chimie (sciences) > Chimie organique de synthèse - Centre de recherches du cyclotron >]
Publication date :	Jun-2010
Audience :	International
Event name :	FACS XIII - French American Chemical Society
Event date :	du 6 juin 2010 au 10 juin 2010
Event organizer :	Jean Suffert, Robert Dodd, Gaelle Blond, Gary Molander, Bruce Lipshutz
Event place (city) :	Obernai
Event country :	France
Abstract :	[en] Oligonucleotides (ONs), especially small interfering RNA (siRNA), are promising therapeutic agents, but their pharmacokinetics and biodistributions are widely unknown. Positron Emission Tomography (PET) using fluorine-18 is a suitable technique to image and quantify such biological processes. The challenge for the radiochemist is to introduce this short half-life isotope (t1/2(18F)=109.7 min) onto oligonucleotides or, more generally, biomolecules. The most common technique requires the coupling of a prosthetic group bearing the radiotracer with the biomolecule. Current methods for labeling ONs with fluorine-18 have sub-optimal yields and require a long synthesis time.1 Click chemistry, e.g. 1,3-dipolar Huisgen cycloaddition of azides to alkynes, could be an efficient way to increase yields and reduce synthesis time. Conjugations with ONs are usually performed at 3’-ends using a well-chosen linker in order to limit degradation by exonucleases and to avoid alteration of hybridization properties and siRNA gene silencing efficiency. This also allows the development of universal solid supports used for the solidphase synthesis of ONs. Here we report the synthesis of three alkyne-bearing linkers , the synthesis and radiosynthesis of the complementary azido-bearing prosthetic groups (1-(azidomethyl)-4-[18F]- fluorobenzene) and coupling with functionalized ONs.
Permalink :	http://hdl.handle.net/2268/62864

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	File	Commentary	Version	Size	Access
Restricted access	GK_FACSv2.pdf	Poster	Publisher postprint	1.02 MB	Request copy
Restricted access	KAISIN_Abstract.pdf	Abstract	Publisher postprint	379.89 kB	Request copy

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