title: Synthesis and evaluation of a fluorine-18 labeled antisense oligonucleotide as a potential PET tracer for iNOS mRNA expression.
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.
authors.affiliation: PET Center, Groningen University Hospital, P.O. Box 30.001, 9700 RB Groningen, The Netherlands. e.f.j.de.vries@pet.azg.nl
authors.forename: Erik F J
authors.initials: EF
authors.lastname: de Vries
authors.forename: Joke
authors.initials: J
authors.lastname: Vroegh
authors.forename: Gerard
authors.initials: G
authors.lastname: Dijkstra
authors.forename: Han
authors.initials: H
authors.lastname: Moshage
authors.forename: Philip H
authors.initials: PH
authors.lastname: Elsinga
authors.forename: Peter L M
authors.initials: PL
authors.lastname: Jansen
authors.forename: Willem
authors.initials: W
authors.lastname: Vaalburg
mesh_terms: D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000000981:diagnostic imaging* / Q000235:genetics / Q000378:metabolism*; D005240:Feasibility Studies; D005462:Fluorine Radioisotopes / Q000493:pharmacokinetics; D020869:Gene Expression Profiling / Q000379:methods; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D019001:Nitric Oxide Synthase / Q000235:genetics* / Q000378:metabolism*; D052247:Nitric Oxide Synthase Type II; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D049268:Positron-Emission Tomography / Q000379:methods; D012333:RNA, Messenger / Q000378:metabolism*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics
chemical_list: D005462:Fluorine Radioisotopes; D016376:Oligonucleotides, Antisense; D012333:RNA, Messenger; D019275:Radiopharmaceuticals; C496319:NOS2 protein, human; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II