Key result
C-5 propyne 2'-deoxy phosphorothioate oligonucleotides completely blocked T antigen translation when injected into the nucleus, whereas 2'-O-allyl phosphodiester oligonucleotides were 20-fold less active.
Population
Cellular and in vitro models evaluating SV40 large T antigen translation
Design
Preclinical
Authors
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May inform antisense oligo design to boost nuclear hybridization rates; leaves open clinical translation from animal data.
C-5 propyne 2'-deoxy phosphorothioate oligonucleotides effectively prevent mRNA translation once hybridized, suggesting future improvements require increasing the rate of complex formation in the nucleus rather than complex stability.
Moulds et al. (1995) studied this question. C-5 propyne oligonucleotides vs. C-5 propyne 2'-O-allyl phosphodiester ONs was evaluated on Antisense inhibition of protein synthesis. C-5 propyne 2'-deoxy phosphorothioate oligonucleotides completely blocked T antigen translation when injected into the nucleus, whereas 2'-O-allyl phosphodiester oligonucleotides were 20-fold less active.
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