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Synthesis and properties of radiolabeled CPTA–oligonucleotides

✍ Scribed by S. Wagner; R. Eritja; M. Zuhayra; F. Oberdorfer; A. Mohammed; W. Mier; U. Haberkorn; M. Eisenhut

Publisher
John Wiley and Sons
Year
2003
Tongue
French
Weight
140 KB
Volume
46
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A solid phase technique for the preparation of antisense oligodeoxynucleotides (ODNs) is described featuring 5′‐end conjugated 4‐[(1,4,8,11‐tetraazacyclotet‐radec‐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′‐protected and 3′‐unprotected ODNs. Propane‐1,3‐diol 3′‐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′‐end. Copyright © 2002 John Wiley & Sons, Ltd.

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