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Mechanisms of single-stranded phosphorothioate modified antisense oligonucleotide accumulation in hepatocytes.

Koller E, Vincent TM, Chappell A, De S, Manoharan M, Bennett CF.

Nucleic Acids Res. 2011 Jun;39(11):4795-807. doi: 10.1093/nar/gkr089. Epub 2011 Feb 23.


Asialoglycoprotein receptor 1 mediates productive uptake of N-acetylgalactosamine-conjugated and unconjugated phosphorothioate antisense oligonucleotides into liver hepatocytes.

Tanowitz M, Hettrick L, Revenko A, Kinberger GA, Prakash TP, Seth PP.

Nucleic Acids Res. 2017 Dec 1;45(21):12388-12400. doi: 10.1093/nar/gkx960.


Pharmacokinetics and pharmacodynamics of an antisense phosphorothioate oligonucleotide targeting Fas mRNA in mice.

Yu RZ, Zhang H, Geary RS, Graham M, Masarjian L, Lemonidis K, Crooke R, Dean NM, Levin AA.

J Pharmacol Exp Ther. 2001 Feb;296(2):388-95.


Characterizing the effect of GalNAc and phosphorothioate backbone on binding of antisense oligonucleotides to the asialoglycoprotein receptor.

Schmidt K, Prakash TP, Donner AJ, Kinberger GA, Gaus HJ, Low A, Østergaard ME, Bell M, Swayze EE, Seth PP.

Nucleic Acids Res. 2017 Mar 17;45(5):2294-2306. doi: 10.1093/nar/gkx060.


Co-Administration of an Excipient Oligonucleotide Helps Delineate Pathways of Productive and Nonproductive Uptake of Phosphorothioate Antisense Oligonucleotides in the Liver.

Donner AJ, Wancewicz EV, Murray HM, Greenlee S, Post N, Bell M, Lima WF, Swayze EE, Seth PP.

Nucleic Acid Ther. 2017 Aug;27(4):209-220. doi: 10.1089/nat.2017.0662. Epub 2017 Apr 27.


2'-O-[2-[(N,N-dimethylamino)oxy]ethyl]-modified oligonucleotides inhibit expression of mRNA in vitro and in vivo.

Prakash TP, Johnston JF, Graham MJ, Condon TP, Manoharan M.

Nucleic Acids Res. 2004 Feb 3;32(2):828-33. Print 2004.


Stabilin-1 and Stabilin-2 are specific receptors for the cellular internalization of phosphorothioate-modified antisense oligonucleotides (ASOs) in the liver.

Miller CM, Donner AJ, Blank EE, Egger AW, Kellar BM, Østergaard ME, Seth PP, Harris EN.

Nucleic Acids Res. 2016 Apr 7;44(6):2782-94. doi: 10.1093/nar/gkw112. Epub 2016 Feb 22.


TCP1 complex proteins interact with phosphorothioate oligonucleotides and can co-localize in oligonucleotide-induced nuclear bodies in mammalian cells.

Liang XH, Shen W, Sun H, Prakash TP, Crooke ST.

Nucleic Acids Res. 2014 Jul;42(12):7819-32. doi: 10.1093/nar/gku484. Epub 2014 May 26.


2'-Fluoro-modified phosphorothioate oligonucleotide can cause rapid degradation of P54nrb and PSF.

Shen W, Liang XH, Sun H, Crooke ST.

Nucleic Acids Res. 2015 May 19;43(9):4569-78. doi: 10.1093/nar/gkv298. Epub 2015 Apr 8.


Antisense inhibition of human telomerase by phosphorothioate oligonucleotide-peptide conjugates.

Diala I, Murao S, Fujii M.

Nucleic Acids Symp Ser (Oxf). 2008;(52):679-80. doi: 10.1093/nass/nrn343.


Clathrin and caveolin-1 expression in primary pigmented rabbit conjunctival epithelial cells: role in PLGA nanoparticle endocytosis.

Qaddoumi MG, Gukasyan HJ, Davda J, Labhasetwar V, Kim KJ, Lee VH.

Mol Vis. 2003 Oct 15;9:559-68.


Intra-endosomal trafficking mediated by lysobisphosphatidic acid contributes to intracellular release of phosphorothioate-modified antisense oligonucleotides.

Wang S, Sun H, Tanowitz M, Liang XH, Crooke ST.

Nucleic Acids Res. 2017 May 19;45(9):5309-5322. doi: 10.1093/nar/gkx231.


Cellular uptake mechanism for oligonucleotides: involvement of endocytosis in the uptake of phosphodiester oligonucleotides by a human colorectal adenocarcinoma cell line, HCT-15.

Nakai D, Seita T, Terasaki T, Iwasa S, Shoji Y, Mizushima Y, Sugiyama Y.

J Pharmacol Exp Ther. 1996 Sep;278(3):1362-72.


Antisense vasopressin oligonucleotides: uptake, turnover, distribution, toxicity and behavioral effects.

Meeker R, LeGrand G, Ramirez J, Smith T, Shih YH.

J Neuroendocrinol. 1995 Jun;7(6):419-28.


Human T-cell leukemia virus type I tax transformation is associated with increased uptake of oligodeoxynucleotides in vitro and in vivo.

Kitajima I, Shinohara T, Minor T, Bibbs L, Bilakovics J, Nerenberg M.

J Biol Chem. 1992 Dec 25;267(36):25881-8.


Gene silencing in mammalian cells with light-activated antisense agents.

Young DD, Lusic H, Lively MO, Yoder JA, Deiters A.

Chembiochem. 2008 Dec 15;9(18):2937-40. doi: 10.1002/cbic.200800627. No abstract available.


In vitro and in vivo transport and delivery of phosphorothioate oligonucleotides with cationic liposomes.

Miyano-Kurosaki N, Barnor JS, Takeuchi H, Owada T, Nakashima H, Yamamoto N, Matsuzaki T, Shimada F, Takaku H.

Antivir Chem Chemother. 2004 Mar;15(2):93-100.


Protamine-fragment peptides fused to an SV40 nuclear localization signal deliver oligonucleotides that produce antisense effects in prostate and bladder carcinoma cells.

Benimetskaya L, Guzzo-Pernell N, Liu ST, Lai JC, Miller P, Stein CA.

Bioconjug Chem. 2002 Mar-Apr;13(2):177-87.


Nucleic acid binding proteins affect the subcellular distribution of phosphorothioate antisense oligonucleotides.

Bailey JK, Shen W, Liang XH, Crooke ST.

Nucleic Acids Res. 2017 Oct 13;45(18):10649-10671. doi: 10.1093/nar/gkx709.

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