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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Dades bibliogràfiques
Publicat a:Nucleic Acids Res
Autors principals: 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
Idioma:Inglês
Publicat: Oxford University Press 2019
Matèries:
Chemical Biology and Nucleic Acid Chemistry
Accés en línia: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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