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Items: 42


Fatty acid conjugation enhances potency of antisense oligonucleotides in muscle.

Prakash TP, Mullick AE, Lee RG, Yu J, Yeh ST, Low A, Chappell AE, Østergaard ME, Murray S, Gaus HJ, Swayze EE, Seth PP.

Nucleic Acids Res. 2019 Jul 9;47(12):6029-6044. doi: 10.1093/nar/gkz354.


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

Østergaard ME, Jackson M, Low A, E Chappell A, G Lee R, Peralta RQ, Yu J, Kinberger GA, Dan A, Carty R, Tanowitz M, Anderson P, Kim TW, Fradkin L, Mullick AE, Murray S, Rigo F, Prakash TP, Bennett CF, Swayze EE, Gaus HJ, Seth PP.

Nucleic Acids Res. 2019 Jul 9;47(12):6045-6058. doi: 10.1093/nar/gkz360.


Characterization of the interactions of chemically-modified therapeutic nucleic acids with plasma proteins using a fluorescence polarization assay.

Gaus HJ, Gupta R, Chappell AE, Østergaard ME, Swayze EE, Seth PP.

Nucleic Acids Res. 2019 Feb 20;47(3):1110-1122. doi: 10.1093/nar/gky1260.


Huntingtin suppression restores cognitive function in a mouse model of Huntington's disease.

Southwell AL, Kordasiewicz HB, Langbehn D, Skotte NH, Parsons MP, Villanueva EB, Caron NS, Østergaard ME, Anderson LM, Xie Y, Cengio LD, Findlay-Black H, Doty CN, Fitsimmons B, Swayze EE, Seth PP, Raymond LA, Frank Bennett C, Hayden MR.

Sci Transl Med. 2018 Oct 3;10(461). pii: eaar3959. doi: 10.1126/scitranslmed.aar3959.


Studies directed toward the asialoglycoprotein receptor mediated delivery of 5-fluoro-2'-deoxyuridine for hepatocellular carcinoma.

Rico L, Østergaard ME, Bell M, Seth PP, Hanessian S.

Bioorg Med Chem Lett. 2018 Aug 15;28(15):2652-2654. doi: 10.1016/j.bmcl.2018.06.002. Epub 2018 Jun 1.


Fluorinated Nucleotide Modifications Modulate Allele Selectivity of SNP-Targeting Antisense Oligonucleotides.

Østergaard ME, Nichols J, Dwight TA, Lima W, Jung ME, Swayze EE, Seth PP.

Mol Ther Nucleic Acids. 2017 Jun 16;7:20-30. doi: 10.1016/j.omtn.2017.02.001. Epub 2017 Feb 9.


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.


A novel humanized mouse model of Huntington disease for preclinical development of therapeutics targeting mutant huntingtin alleles.

Southwell AL, Skotte NH, Villanueva EB, Østergaard ME, Gu X, Kordasiewicz HB, Kay C, Cheung D, Xie Y, Waltl S, Dal Cengio L, Findlay-Black H, Doty CN, Petoukhov E, Iworima D, Slama R, Ooi J, Pouladi MA, Yang XW, Swayze EE, Seth PP, Hayden MR.

Hum Mol Genet. 2017 Mar 15;26(6):1115-1132. doi: 10.1093/hmg/ddx021.


Synthesis and biological evaluation of sialyl-oligonucleotide conjugates targeting leukocyte B trans-membranal receptor CD22 as delivery agents for nucleic acid drugs.

St-Pierre G, Pal S, Østergaard ME, Zhou T, Yu J, Tanowitz M, Seth PP, Hanessian S.

Bioorg Med Chem. 2016 Jun 1;24(11):2397-409. doi: 10.1016/j.bmc.2016.03.047. Epub 2016 Mar 29.


A convenient synthesis of 5'-triantennary N-acetyl-galactosamine clusters based on nitromethanetrispropionic acid.

Migawa MT, Prakash TP, Vasquez G, Wan WB, Yu J, Kinberger GA, Østergaard ME, Swayze EE, Seth PP.

Bioorg Med Chem Lett. 2016 May 1;26(9):2194-7. doi: 10.1016/j.bmcl.2016.03.070. Epub 2016 Mar 17.


Comprehensive Structure-Activity Relationship of Triantennary N-Acetylgalactosamine Conjugated Antisense Oligonucleotides for Targeted Delivery to Hepatocytes.

Prakash TP, Yu J, Migawa MT, Kinberger GA, Wan WB, Østergaard ME, Carty RL, Vasquez G, Low A, Chappell A, Schmidt K, Aghajan M, Crosby J, Murray HM, Booten SL, Hsiao J, Soriano A, Machemer T, Cauntay P, Burel SA, Murray SF, Gaus H, Graham MJ, Swayze EE, Seth PP.

J Med Chem. 2016 Mar 24;59(6):2718-33. doi: 10.1021/acs.jmedchem.5b01948. Epub 2016 Mar 9.


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.


Design, synthesis, and duplex-stabilizing properties of conformationally constrained tricyclic analogues of LNA.

Giacometti RD, Salinas JC, Østergaard ME, Swayze EE, Seth PP, Hanessian S.

Org Biomol Chem. 2016 Feb 14;14(6):2034-40. doi: 10.1039/c5ob02576a.


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

Prakash TP, Brad Wan W, Low A, Yu J, Chappell AE, Gaus H, Kinberger GA, Østergaard ME, Migawa MT, Swayze EE, Seth PP.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4127-30. doi: 10.1016/j.bmcl.2015.08.019. Epub 2015 Aug 8.


Allele-Selective Inhibition of Mutant Huntingtin with 2-Thio- and C5- Triazolylphenyl-Deoxythymidine-Modified Antisense Oligonucleotides.

Østergaard ME, Kumar P, Nichols J, Watt A, Sharma PK, Nielsen P, Seth PP.

Nucleic Acid Ther. 2015 Oct;25(5):266-74. doi: 10.1089/nat.2015.0547. Epub 2015 Jul 29.


Efficient Synthesis and Biological Evaluation of 5'-GalNAc Conjugated Antisense Oligonucleotides.

Østergaard ME, Yu J, Kinberger GA, Wan WB, Migawa MT, Vasquez G, Schmidt K, Gaus HJ, Murray HM, Low A, Swayze EE, Prakash TP, Seth PP.

Bioconjug Chem. 2015 Aug 19;26(8):1451-5. doi: 10.1021/acs.bioconjchem.5b00265. Epub 2015 Jun 10.


HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity.

Mattis VB, Tom C, Akimov S, Saeedian J, Østergaard ME, Southwell AL, Doty CN, Ornelas L, Sahabian A, Lenaeus L, Mandefro B, Sareen D, Arjomand J, Hayden MR, Ross CA, Svendsen CN.

Hum Mol Genet. 2015 Jun 1;24(11):3257-71. doi: 10.1093/hmg/ddv080. Epub 2015 Mar 3.


Biophysical and biological characterization of hairpin and molecular beacon RNase H active antisense oligonucleotides.

Østergaard ME, Thomas G, Koller E, Southwell AL, Hayden MR, Seth PP.

ACS Chem Biol. 2015 May 15;10(5):1227-33. doi: 10.1021/cb500880f. Epub 2015 Feb 13.


Allele-specific suppression of mutant huntingtin using antisense oligonucleotides: providing a therapeutic option for all Huntington disease patients.

Skotte NH, Southwell AL, Østergaard ME, Carroll JB, Warby SC, Doty CN, Petoukhov E, Vaid K, Kordasiewicz H, Watt AT, Freier SM, Hung G, Seth PP, Bennett CF, Swayze EE, Hayden MR.

PLoS One. 2014 Sep 10;9(9):e107434. doi: 10.1371/journal.pone.0107434. eCollection 2014.


Comparison of duplex stabilizing properties of 2'-fluorinated nucleic acid analogues with furanose and non-furanose sugar rings.

Østergaard ME, Dwight T, Berdeja A, Swayze EE, Jung ME, Seth PP.

J Org Chem. 2014 Sep 19;79(18):8877-81. doi: 10.1021/jo501381q. Epub 2014 Aug 27.


In vivo evaluation of candidate allele-specific mutant huntingtin gene silencing antisense oligonucleotides.

Southwell AL, Skotte NH, Kordasiewicz HB, Østergaard ME, Watt AT, Carroll JB, Doty CN, Villanueva EB, Petoukhov E, Vaid K, Xie Y, Freier SM, Swayze EE, Seth PP, Bennett CF, Hayden MR.

Mol Ther. 2014 Dec;22(12):2093-106. doi: 10.1038/mt.2014.153. Epub 2014 Aug 7.


Differential effects on allele selective silencing of mutant huntingtin by two stereoisomers of α,β-constrained nucleic acid.

Østergaard ME, Gerland B, Escudier JM, Swayze EE, Seth PP.

ACS Chem Biol. 2014 Sep 19;9(9):1975-9. doi: 10.1021/cb5003027. Epub 2014 Jul 25.


Synthesis and duplex-stabilizing properties of fluorinated N-methanocarbathymidine analogues locked in the C3'-endo conformation.

Jung ME, Dwight TA, Vigant F, Østergaard ME, Swayze EE, Seth PP.

Angew Chem Int Ed Engl. 2014 Sep 8;53(37):9893-7. doi: 10.1002/anie.201405283. Epub 2014 Jul 15.


Synthesis and biophysical properties of C5-functionalized LNA (locked nucleic acid).

Kumar P, Østergaard ME, Baral B, Anderson BA, Guenther DC, Kaura M, Raible DJ, Sharma PK, Hrdlicka PJ.

J Org Chem. 2014 Jun 6;79(11):5047-61. doi: 10.1021/jo500614a. Epub 2014 May 13.


C5-alkynyl-functionalized α-L-LNA: synthesis, thermal denaturation experiments and enzymatic stability.

Kumar P, Baral B, Anderson BA, Guenther DC, Østergaard ME, Sharma PK, Hrdlicka PJ.

J Org Chem. 2014 Jun 6;79(11):5062-73. doi: 10.1021/jo5006153. Epub 2014 May 13.


Rational design of antisense oligonucleotides targeting single nucleotide polymorphisms for potent and allele selective suppression of mutant Huntingtin in the CNS.

Østergaard ME, Southwell AL, Kordasiewicz H, Watt AT, Skotte NH, Doty CN, Vaid K, Villanueva EB, Swayze EE, Bennett CF, Hayden MR, Seth PP.

Nucleic Acids Res. 2013 Nov;41(21):9634-50. doi: 10.1093/nar/gkt725. Epub 2013 Aug 19.


A constrained tricyclic nucleic acid analogue of α-L-LNA: investigating the effects of dual conformational restriction on duplex thermal stability.

Hanessian S, Wagger J, Merner BL, Giacometti RD, Ostergaard ME, Swayze EE, Seth PP.

J Org Chem. 2013 Sep 20;78(18):9064-75. doi: 10.1021/jo401170y. Epub 2013 Sep 4.


Synthesis and antisense properties of fluoro cyclohexenyl nucleic acid (F-CeNA), a nuclease stable mimic of 2'-fluoro RNA.

Seth PP, Yu J, Jazayeri A, Pallan PS, Allerson CR, Østergaard ME, Liu F, Herdewijn P, Egli M, Swayze EE.

J Org Chem. 2012 Jun 1;77(11):5074-85. doi: 10.1021/jo300594b. Epub 2012 May 18.


Structural requirements for hybridization at the 5'-position are different in α-l-LNA as compared to β-D-LNA.

Seth PP, Allerson CR, Ostergaard ME, Swayze EE.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):296-9. doi: 10.1016/j.bmcl.2011.11.012. Epub 2011 Nov 11.


Synthesis and biophysical evaluation of 3'-Me-α-L-LNA - Substitution in the minor groove of α-L-LNA duplexes.

Seth PP, Allerson CA, Østergaard ME, Swayze EE.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4690-4. doi: 10.1016/j.bmcl.2011.06.104. Epub 2011 Jun 30.


Pyrene intercalating nucleic acids with a carbon linker.

Østergaard ME, Wamberg MC, Pedersen EB.

Nucleosides Nucleotides Nucleic Acids. 2011 Mar;30(3):210-26. doi: 10.1080/15257770.2011.567202.


Pyrene-functionalized oligonucleotides and locked nucleic acids (LNAs): tools for fundamental research, diagnostics, and nanotechnology.

Østergaard ME, Hrdlicka PJ.

Chem Soc Rev. 2011 Dec;40(12):5771-88. doi: 10.1039/c1cs15014f. Epub 2011 Apr 13. Review.


Preparation of C5-functionalized locked nucleic acids (LNAs).

Kumar P, Østergaard ME, Hrdlicka PJ.

Curr Protoc Nucleic Acid Chem. 2011 Mar;Chapter 4:Unit 4.43. doi: 10.1002/0471142700.nc0443s44.


C5-functionalized DNA, LNA, and α-L-LNA: positional control of polarity-sensitive fluorophores leads to improved SNP-typing.

Østergaard ME, Kumar P, Baral B, Guenther DC, Anderson BA, Ytreberg FM, Deobald L, Paszczynski AJ, Sharma PK, Hrdlicka PJ.

Chemistry. 2011 Mar 7;17(11):3157-65. doi: 10.1002/chem.201002109. Epub 2011 Feb 15.


Novel insights into the use of Glowing LNA as nucleic acid detection probes--influence of labeling density and nucleobases.

Østergaard ME, Maity J, Babu BR, Wengel J, Hrdlicka PJ.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7265-8. doi: 10.1016/j.bmcl.2010.10.089. Epub 2010 Nov 9.


Glowing locked nucleic acids: brightly fluorescent probes for detection of nucleic acids in cells.

Østergaard ME, Cheguru P, Papasani MR, Hill RA, Hrdlicka PJ.

J Am Chem Soc. 2010 Oct 13;132(40):14221-8. doi: 10.1021/ja1057295.


Pyrene-functionalized triazole-linked 2'-deoxyuridines-probes for discrimination of single nucleotide polymorphisms (SNPs).

Østergaard ME, Guenther DC, Kumar P, Baral B, Deobald L, Paszczynski AJ, Sharma PK, Hrdlicka PJ.

Chem Commun (Camb). 2010 Jul 21;46(27):4929-31. doi: 10.1039/c0cc01133a. Epub 2010 Jun 4.


Optimized DNA-targeting using triplex forming C5-alkynyl functionalized LNA.

Sau SP, Kumar P, Anderson BA, Østergaard ME, Deobald L, Paszczynski A, Sharma PK, Hrdlicka PJ.

Chem Commun (Camb). 2009 Nov 28;(44):6756-8. doi: 10.1039/b917312a. Epub 2009 Oct 12.


C5-functionalized LNA: unparalleled hybridization properties and enzymatic stability.

Østergaard ME, Kumar P, Baral B, Raible DJ, Kumar TS, Anderson BA, Guenther DC, Deobald L, Paszczynski AJ, Sharma PK, Hrdlicka PJ.

Chembiochem. 2009 Nov 23;10(17):2740-3. doi: 10.1002/cbic.200900500. No abstract available.


Parallel RNA-strand recognition by 2'-amino-beta-L-LNA.

Kumar TS, Ostergaard ME, Sharma PK, Nielsen P, Wengel J, Hrdlicka PJ.

Bioorg Med Chem Lett. 2009 May 1;19(9):2396-9. doi: 10.1016/j.bmcl.2009.03.079. Epub 2009 Mar 24.


Functionalized 2'-amino-alpha-L-LNA: directed positioning of intercalators for DNA targeting.

Kumar TS, Madsen AS, Østergaard ME, Sau SP, Wengel J, Hrdlicka PJ.

J Org Chem. 2009 Feb 6;74(3):1070-81. doi: 10.1021/jo802037v.


Nucleic acid structural engineering using pyrene-functionalized 2'-amino-alpha-L-LNA monomers and abasic sites.

Kumar TS, Madsen AS, Østergaard ME, Wengel J, Hrdlicka PJ.

J Org Chem. 2008 Sep 19;73(18):7060-6. doi: 10.1021/jo800551j. Epub 2008 Aug 19.


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