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Labelled oligonucleotides as radiopharmaceuticals: pitfalls, problems and perspectives
Cheraz Khélifi Younes1, Raphaël Boisgard, Bertrand Tavitian
1Laboratoire d imagerie de l expression des genes, Inserm Erit-M0103, Cea/Dsv/Shfj, 4 place du g n ral Leclerc, Orsay cedex, 91401, France. tavitian@shfj.cea.fr
Current Pharmaceutical Design
|June 8, 2002
Summary
Radiolabeled oligonucleotides show promise for gene imaging, cancer therapy, and diagnostics. Despite inherent pharmaceutical limitations, modified oligonucleotides offer improved stability and therapeutic potential for early disease detection and cancer treatment.
Area of Science:
- Biomedical imaging and targeted therapy
- Radiopharmaceutical development
- Molecular diagnostics
Background:
- Single-stranded oligonucleotides can be labeled with radioisotopes to create radiopharmaceuticals.
- Oligonucleotides have potential applications in gene imaging, monitoring chemotherapy, gene radiotherapy, and protein target imaging.
- Challenges with native oligonucleotides include poor stability, membrane passage, and side effects.
Purpose of the Study:
- To explore the development and applications of radiolabeled oligonucleotides as radiopharmaceuticals.
- To highlight the potential of modified oligonucleotides as improved therapeutic and diagnostic agents.
- To discuss the role of imaging techniques in advancing oligonucleotide-based therapies.
Main Methods:
- Labeling of single-stranded oligonucleotides with positron or single-photon emitters.
- Development of chemically modified oligonucleotides (e.g., phosphorothioate, methylphosphonate, peptide nucleic acid oligomers).
- Utilizing aptamer oligonucleotides for protein target imaging and pre-targeting strategies.
Main Results:
- Radiolabeled oligonucleotides demonstrate potential for in vivo gene expression imaging and monitoring antisense chemotherapy.
- Modified oligonucleotides show promise in clinical trials for cancer chemotherapy.
- Various radioisotopes (e.g., Tc-99m, In-111, C-11, F-18) have been successfully used for labeling oligonucleotides.
Conclusions:
- Radiolabeled oligonucleotides represent a versatile platform for molecular imaging and targeted therapy.
- Chemically modified oligonucleotides offer enhanced pharmaceutical properties, overcoming limitations of native DNA.
- Oligonucleotide-based radiopharmaceuticals hold significant potential for early disease detection, cancer diagnosis, and personalized medicine.