Antisense Gapmers with LNA-Wings and (S)-5'-C-Aminopropyl-2'-arabinofluoro-nucleosides Could Efficiently Suppress the Expression of KNTC2.

ABSTRACT: Previously reported (S)-5'-C-aminopropyl-2'-arabinofluoro-thymidine (5ara-T) and newly synthesized (S)-5'-C-aminopropyl-2'-arabinofluoro-5-methyl-cytidine (5ara-^MeC) analogs were incorporated into a series of antisense gapmers containing multiple phosphorothioate (PS) linkages and locked nucleic acids (LNAs) in their wing regions. The functional properties of the gapmers were further evaluated in vitro. Compared with the positive control, for the LNA-wing full PS gapmer without 5ara modification, it was revealed that each gapmer could have a high affinity and be thermally stable under biological conditions. Although the cleavage pattern was obviously changed; gapmers with 5ara modification could still efficiently activate <

SUBMITTER: Zhou Y 

PROVIDER: S-EPMC9654562 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature