Development of a lyophilized kit formulation for labeling of DNA probes with 99mTc

Hjelstuen, O.; Sætern, Ann Mari; Tønnesen, H. Hjorth; Bremer, P. O.; Verbruggen, A.

doi:10.1016/s0378-5173(99)00293-8

Cited by 4 publications

(1 citation statement)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The complex had a radiochemical purity of more than 97% with specific activity of about 2.8Ci/μmol [28]. Later on Hjelstuen and colleagues from the same group reported the development of the first kit for one-step labeling of oligonucleotides with 99m Tc using S -benzoyl-mercaptoacetyldiglycine (MAG 2 ) [29]. In a study aimed at evaluating the antisense targeting properties of locked nucleic acid (LNA) a study with 99m Tc labeled LNA was undertaken in Hnatowich’s laboratory [30].…”

Section: ) Probe Development For Antisense Imagingmentioning

confidence: 99%

Radiolabeled Oligonucleotides for Antisense Imaging

Iyer¹,

He²

2011

COS

View full text Add to dashboard Cite

Oligonucleotides radiolabeled with isotopes emitting γ-rays (for SPECT imaging) or positrons (for PET imaging) can be useful for targeting messenger RNA (mRNA) thereby serving as non-invasive imaging tools for detection of gene expression in vivo (antisense imaging). Radiolabeled oligonucleotides may also be used for monitoring their in vivo fate, thereby helping us better understand the barriers to its delivery for antisense targeting. These developments have led to a new area of molecular imaging and targeting, utilizing radiolabeled antisense oligonucleotides. However, the success of antisense imaging relies heavily on overcoming the barriers for its targeted delivery in vivo. Furthermore, the low ability of the radiolabeled antisense oligonucleotide to subsequently internalize into the cell and hybridize with its target mRNA poses additional challenges in realizing its potentials. This review covers the advances in the antisense imaging probe development for PET and SPECT, with an emphasis on radiolabeling strategies, stability, delivery and in vivo targeting.

show abstract

Section: ) Probe Development For Antisense Imagingmentioning

confidence: 99%

Radiolabeled Oligonucleotides for Antisense Imaging

Iyer¹,

He²

2011

COS

View full text Add to dashboard Cite

show abstract

Aptamers: a novel class of radiopharmaceutical with diagnostic and therapeutic potential

Guhlke¹,

Famulok

Biersack³

2003

European Journal of Nuclear Medicine and Molecular Imaging

View full text Add to dashboard Cite

Initial investigations of 99mTc-labeled morpholinos for radiopharmaceutical applications

et al. 2001

View full text Add to dashboard Cite

This laboratory is evaluating phosphorothioate deoxyribonucleic acids (DNAs) and peptide nucleic acids (PNAs) for a variety of nuclear medicine applications. Morpholinos (MORFs) are a new class of oligomers with a nuclease-resistant, nonionic and water-soluble phosphorodiamidate backbone. We now report on the in vitro and in vivo properties of MORFs labeled with technetium-99m. Both 15-mer and 18-mer MORFs were obtained, each with a primary amine attached to the 3' equivalent end via a three-carbon beta-alanine linker. The amine was used to conjugate with NHS-MAG3 for 99mTc radiolabeling. By surface plasmon resonance at room temperature, the association rate constant for hybridization of the 18-mer MORF to its complementary oligomer (cMORF) was equivalent to that of DNAs and PNAs of comparable length. Hybridization of 99mTc-MORF in vitro to free cMORF, to a cMORF polymer and to cMORF beads was nearly quantitative under a variety of conditions. Kinetic studies in vitro at room temperature showed rapid (2-5 min) and nearly quantitative (90%) binding to cMORF beads. Using size-exclusion high-performance liquid chromatography, the stability of the 99mTc-MORF was found to be greater than 85% over 24 h in 37 degrees C serum with minimal protein binding. In normal mice, the 99mTc-MORF showed rapid pharmacokinetics, with only 21% and 8% remaining in the whole body at 3 and 24 h post administration, respectively. In vivo targeting with 99mTc-MORF of cMORF beads in one thigh of normal mice compared to control beads in the other thigh showed target/control thigh ratios of 2-10 between 3 and 24 h. These results demonstrate that MORF oligomers are capable of in vivo hybridization. Their properties of hybridization affinity and kinetics and their in vivo stability and pharmacokinetics make them suitable subjects for in vivo studies.

show abstract

Development of a lyophilized kit formulation for labeling of DNA probes with 99mTc

Cited by 4 publications

References 12 publications

Radiolabeled Oligonucleotides for Antisense Imaging

Radiolabeled Oligonucleotides for Antisense Imaging

Aptamers: a novel class of radiopharmaceutical with diagnostic and therapeutic potential

Initial investigations of 99mTc-labeled morpholinos for radiopharmaceutical applications

Contact Info

Product

Resources

About