Skip to main content
SLU publication database (SLUpub)

Research article2004Peer reviewed

Synthesis, physicochemical and biochemical studies of 1',2'-oxetane constrained adenosine and guanosine modified oligonucleotides, and their comparison with those of the corresponding cytidine and thymidine analogues

Pradeepkumar PI, Cheruku P, Plashkevych O, Acharya P, Gohil S, Chattopadhyaya J


We have earlier reported the synthesis and antisense properties of the conformationally constrained oxetane-C and -T containing oligonucleotides, which have shown effective down-regulation of the proto-oncogene c-myb mRNA in the K562 human leukemia cells. Here we report on the straightforward syntheses of the oxetane-A and oxetane-G nucleosides as well as their incorporations into antisense oligonucleotides (AONs), and compare their structural and antisense properties with those of the T and C modified AONs (including the thermostability and RNase H recruitment capability of the AON/RNA hybrid duplex by Michaelis-Menten kinetic analyses, their resistance in the human serum, as well as in the presence of exo and endonucleases)

Published in

Journal of the American Chemical Society
2004, Volume: 126, number: 37, pages: 11484-11499

    Publication identifier


    Permanent link to this page (URI)