title: Aptamers as radiopharmaceuticals for nuclear imaging and therapy.
abstract: Today, radiopharmaceuticals belong to the standard instrumentation of nuclear medicine, both in the context of diagnosis and therapy. The majority of radiopharmaceuticals consist of targeting biomolecules which are designed to interact with a disease-related molecular target. A plethora of targeting biomolecules of radiopharmaceuticals exists, including antibodies, antibody fragments, proteins, peptides and nucleic acids. Nucleic acids have some significant advantages relative to proteinaceous biomolecules in terms of size, production, modifications, possible targets and immunogenicity. In particular, aptamers (non-coding, synthetic, single-stranded DNA or RNA oligonucleotides) are of interest because they can bind a molecular target with high affinity and specificity. At present, few aptamers have been investigated preclinically for imaging and therapeutic applications. In this review, we describe the use of aptamers as targeting biomolecules of radiopharmaceuticals. We also discuss the chemical modifications which are needed to turn aptamers into valuable (radio-)pharmaceuticals, as well as the different radiolabeling strategies that can be used to radiolabel oligonucleotides and, in particular, aptamers.
authors.affiliation: Radiobiology Unit, Belgian Nuclear Research Centre (SCK·CEN), Mol, Belgium; Cyclotron Research Centre, University of Liège, Liège, Belgium.
authors.forename: Marlies
authors.initials: M
authors.lastname: Gijs
authors.affiliation: Radiobiology Unit, Belgian Nuclear Research Centre (SCK·CEN), Mol, Belgium.
authors.forename: An
authors.initials: A
authors.lastname: Aerts
authors.affiliation: Radiobiology Unit, Belgian Nuclear Research Centre (SCK·CEN), Mol, Belgium.
authors.forename: Nathalie
authors.initials: N
authors.lastname: Impens
authors.affiliation: Radiobiology Unit, Belgian Nuclear Research Centre (SCK·CEN), Mol, Belgium.
authors.forename: Sarah
authors.initials: S
authors.lastname: Baatout
authors.affiliation: Cyclotron Research Centre, University of Liège, Liège, Belgium. Electronic address: aluxen@ulg.ac.be.
authors.forename: André
authors.initials: A
authors.lastname: Luxen
mesh_terms: D000818:Animals; D052157:Aptamers, Nucleotide / Q000627:therapeutic use*; D003952:Diagnostic Imaging / Q000379:methods*; D006801:Humans; D009683:Nuclear Medicine / Q000379:methods*; D019275:Radiopharmaceuticals / Q000627:therapeutic use*
chemical_list: D052157:Aptamers, Nucleotide; D019275:Radiopharmaceuticals
keywords: Aptamer; Imaging; Nuclear medicine; Radiopharmaceuticals; Therapy