Jacques Lebreton

Comparison of rigid and flexible backbones in antisense oligonucleotides

Abstract Stepwise restriction of free rotation, as well as introduction of positive changes in the internucleosidic linkage are factors which can positively influence the thermal melting behaviour of the corresponding duplexes formed between modified DNA and their RNA complement. By correct positioning of the rigidity within backbone, it is possible to achieve even higher binding affinity (Tms) than with natural oligodeoxyribonucleotides (ODNs).

Comparison of two amides as backbone replacement of the phosphodiester linkage in oligodeoxynucleotides

Abstract The two isomeric amide modifications 1 and 2 show similar effects on the melting temperature of RNA/DNA duplexes, when they replace the natural phosphodiester linkage in the DNA strand. The synthesis of the amide dimer 1 is presented.

Replacement of the phosphodiester linkage in oligonucleotides : comparison of two structural amide isomers

Abstract The two structural amide isomers 2 and 3 as backbone replacement in oligonucleotides lead to very similar results for the binding affinities (Tm) of the duplexes formed with their complementary RNA strands.

Synthesis of Oligodeoxyribonucleotides containing dimers with carbamate moieties as replacement of the natural phosphodiester linkage

Abstract The synthesis of thymidine dimers containing both possible regioisomeric carbamate moieties in place of the natural phosphodiester backbone is described. These dimers were incorporated in oligodeoxyribonucleotides and melting temperatures (T m ) of the DNA/RNA and DNA/DNA duplexes are reported. In addition the nuclease resistance of these single strands were determined.