Solid-phase synthesis of 5′-triantennary N-acetylgalactosamine conjugated antisense oligonucleotides using phosphoramidite chemistry

Bioorganic and Medicinal Chemistry Letters

Volumn 25, Issue 19, 2015, Pages 4127-4130

  Prakash, Thazha P ^a   Brad Wan, W ^a   Low, Audrey ^a   Yu, Jinghua ^a   Chappell, Alfred E ^a   Gaus, Hans ^a   Kinberger, Garth A ^a   Østergaard, Michael E ^a   Migawa, Michael T ^a   Swayze, Eric E ^a   Seth, Punit P ^a  

^a ISIS PHARMACEUTICALS   (United States)

Author keywords

(S) cEt BNA ASO; 5 PGalNAc3; GalNAc conjugation; Hepatocyte targeted delivery

Indexed keywords

ANTISENSE OLIGONUCLEOTIDE; ASIALOGLYCOPROTEIN RECEPTOR; N ACETYLGALACTOSAMINE; PHOSPHORAMIDOUS ACID; MESSENGER RNA; ORGANOPHOSPHORUS COMPOUND; SCARB1 PROTEIN, MOUSE; SCAVENGER RECEPTOR B;

5' UNTRANSLATED REGION; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CELL MEMBRANE; CHEMISTRY; CONJUGATION; CONTROLLED STUDY; DRUG DELIVERY SYSTEM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TOLERABILITY; IC50; LIVER CELL; MOUSE; NONHUMAN; PROTEIN EXPRESSION; QUANTITATIVE ANALYSIS; SOLID PHASE SYNTHESIS; STRUCTURE ACTIVITY RELATION; ANALOGS AND DERIVATIVES; ANIMAL; ANTAGONISTS AND INHIBITORS; DOSE RESPONSE; GENETICS; LIVER; METABOLISM; SYNTHESIS;

ACETYLGALACTOSAMINE; ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; LIVER; MICE; OLIGONUCLEOTIDES, ANTISENSE; ORGANOPHOSPHORUS COMPOUNDS; RNA, MESSENGER; SCAVENGER RECEPTORS, CLASS B; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84944930132     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2015.08.019     Document Type: Article

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