Conjugation of hydrophobic moieties enhances potency of antisense oligonucleotides in the muscle of rodents and non-human primates

We determined the effect of attaching palmitate, tocopherol or cholesterol to PS ASOs and their effects on plasma protein binding and on enhancing ASO potency in the muscle of rodents and monkeys. We found that cholesterol ASO conjugates showed 5-fold potency enhancement in the muscle of rodents rel...

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Bibliografiske detaljer
Udgivet i:Nucleic Acids Res
Main Authors: Østergaard, Michael E, Jackson, Michaela, Low, Audrey, E. Chappell, Alfred, G. Lee, Richard, Peralta, Rachel Q, Yu, Jinghua, Kinberger, Garth A, Dan, Amy, Carty, Rick, Tanowitz, Michael, Anderson, Patrick, Kim, Tae-Won, Fradkin, Linda, Mullick, Adam E, Murray, Sue, Rigo, Frank, Prakash, Thazha P, Bennett, C Frank, Swayze, Eric E, Gaus, Hans J, Seth, Punit P
Format: Artigo
Sprog:Inglês
Udgivet: Oxford University Press 2019
Fag:
Chemical Biology and Nucleic Acid Chemistry
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6614849/
https://ncbi.nlm.nih.gov/pubmed/31076766
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1093/nar/gkz360
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