Consecutive 5'- and 3'-amide linkages stabilise antisense oligonucleotides and elicit an efficient RNase H response.

Epple S., Thorpe C., Baker YR., El-Sagheer AH., Brown T.

Antisense oligonucleotides are now entering the clinic for hard-to-treat diseases. New chemical modifications are urgently required to enhance their drug-like properties. We combine amide coupling with standard oligonucleotide synthesis to assemble backbone chimera gapmers that trigger an efficient RNase H response while improving serum life time and cellular uptake.

DOI

10.1039/d0cc00444h

Type

Journal article

Journal

Chem Commun (Camb)

Publication Date

15/04/2020

Permalink Original publication