Synthesis and evaluation of a fluorine-18 labeled antisense oligonucleotide as a potential PET tracer for iNOS mRNA expression

Nuclear Medicine and Biology
Erik F J de VriesWillem Vaalburg

Abstract

Inducible NO synthase (iNOS) is overexpressed in inflammatory bowel diseases. An antisense oligonucleotide with good hybridization properties for iNOS mRNA was selected using RT-PCR. The oligonucleotide was reliably labeled with fluorine-18 using N-(4-[(18)F]fluorobenzyl)-2-bromoacetamide. Cellular uptake and efflux of oligonucleotide complexed with FuGENE-6 were rapid, unlike naked oligonucleotide, which hardly accumulated. However, neither uptake nor efflux showed any selectivity for iNOS expressing cells. The oligonucleotide showed a high level of non-specific binding, which may have obscured its specific hybridization to iNOS mRNA.

References

Jan 1, 1992·Annual Review of Pharmacology and Toxicology·S T Crooke
Feb 25, 1991·Nucleic Acids Research·J P ShawB Froehler
Apr 1, 1995·The Journal of Clinical Investigation·C BeltingerA M Gewirtz
May 15, 1996·The Journal of Clinical Investigation·E NoiriM S Goligorsky
Apr 18, 1998·Nature Medicine·B TavitianL Di Giamberardino
Oct 18, 2000·Advanced Drug Delivery Reviews·S AkhtarP Sayyed
Jan 10, 2001·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·S Parmentier-BatteurM Plotkine
Oct 19, 2001·Nuclear Medicine Communications·M A Stalteri, S J Mather
Jan 29, 2002·Current Pharmaceutical Design·L SalernoM A Siracusa
Jun 8, 2002·Current Pharmaceutical Design·Cheraz Khélifi YounesBertrand Tavitian

❮ Previous
Next ❯

Citations

Sep 6, 2005·Amino Acids·R Bergmann, J Pietzsch
Oct 2, 2008·European Journal of Nuclear Medicine and Molecular Imaging·Fabien ChauveauBertrand Tavitian
Oct 23, 2014·Therapeutic Delivery·Shubhra Chaturvedi, Anil Kumar Mishra
Jan 10, 2016·Nuclear Medicine and Biology·Marlies GijsAndré Luxen
Jun 16, 2009·Free Radical Biology & Medicine·Hao HongWeibo Cai
Sep 10, 2014·Neuroscience·H AmhaoulS Dedeurwaerdere
Jul 30, 2020·International Journal of Molecular Sciences·Gonçalo S ClementePhilip H Elsinga

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antisense Oligonucleotides: ND

This feed focuses on antisense oligonucleotide therapies such as Inotersen, Nusinursen, and Patisiran, in neurodegenerative diseases including amyotrophic lateral sclerosis.

Related Papers

Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine
Weibo Cai, Xiaoyuan Chen
European Journal of Nuclear Medicine and Molecular Imaging
Weibo CaiXiaoyuan Chen
© 2022 Meta ULC. All rights reserved