A practical method for the synthesis and purification of <sup>14</sup>C labeled oligonucleotides

Sasmor, Henri; Dellinger, Douglas J.; Zenk, Paul C.; Lee, Larry P.

doi:10.1002/jlcr.2580360103

Cited by 5 publications

(1 citation statement)

References 14 publications

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“…In addition, investigation of ODN metabolism and pharmacokinetics would be possible using radiolabeled ODNs. 4,5 For radiolabeling various ligand conjugations have been pursued including diethylenetriamine penta-acetate, 6,7 hydrazinonicotinamide, 8 mercaptoacetyltriglycine, 9 including 111 In and 99m Tc complexation. Using N-(4-[ 18 F]fluorobenzyl)bromoactetamide or the corresponding 76 Br derivative, PET tracers have successfully been introduced to 5 0 -thioate containing ODNs.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and properties of radiolabeled CPTA–oligonucleotides

Wagner

Eritja²,

Zuhayra

et al. 2002

Labelled Comp Radiopharmac

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SummaryA solid phase technique for the preparation of antisense oligodeoxynucleotides (ODNs) is described featuring 5 0 -end conjugated 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)-methyl]benzoic acid (CPTA). Using Fmoc-protected CPTA-C6 amidite, CPTA was conjugated to ODNs at the end of an automated DNA synthesis. To illustrate successful conjugations, the CPTA-ODNs were labeled with 99m Tc using the stannous-chloride reduction method. The resulting 99m Tc complexes showed differences of stability between CPTA-conjugated and CPTA-unconjugated as well as 3 0 -protected and 3 0 -unprotected ODNs. Propane-1,3-diol 3 0 -modification enhanced efficiently the stability of 99m Tc labeled ODN against exonuclease degradation. Fmoc 3 CPTA-C6 amidite turned out to be a versatile ligand for radiometal complexation at the 5 0 -end.

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Section: Introductionmentioning

confidence: 99%