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Items: 1 to 50 of 58

1.

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. 2018 Dec 19. doi: 10.1093/nar/gky1260. [Epub ahead of print]

2.

Structural Determinants for the Interactions of Chemically Modified Nucleic Acids with the Stabilin-2 Clearance Receptor.

Gaus H, Miller CM, Seth PP, Harris EN.

Biochemistry. 2018 Apr 10;57(14):2061-2064. doi: 10.1021/acs.biochem.8b00126. Epub 2018 Mar 30.

3.

Identification of metabolically stable 5΄-phosphate analogs that support single-stranded siRNA activity.

Prakash TP, Lima WF, Murray HM, Li W, Kinberger GA, Chappell AE, Gaus H, Seth PP, Bhat B, Crooke ST, Swayze EE.

Nucleic Acids Res. 2017 Jun 20;45(11):6994. doi: 10.1093/nar/gkx381. No abstract available.

4.

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.

5.

Conjugation of mono and di-GalNAc sugars enhances the potency of antisense oligonucleotides via ASGR mediated delivery to hepatocytes.

Kinberger GA, Prakash TP, Yu J, Vasquez G, Low A, Chappell A, Schmidt K, Murray HM, Gaus H, Swayze EE, Seth PP.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3690-3. doi: 10.1016/j.bmcl.2016.05.084. Epub 2016 May 28.

PMID:
27268307
6.

Elucidation of the Biotransformation Pathways of a Galnac3-conjugated Antisense Oligonucleotide in Rats and Monkeys.

Shemesh CS, Yu RZ, Gaus HJ, Greenlee S, Post N, Schmidt K, Migawa MT, Seth PP, Zanardi TA, Prakash TP, Swayze EE, Henry SP, Wang Y.

Mol Ther Nucleic Acids. 2016 May 10;5:e319. doi: 10.1038/mtna.2016.31.

7.

Pharmacokinetic and Pharmacodynamic Investigations of ION-353382, a Model Antisense Oligonucleotide: Using Alpha-2-Macroglobulin and Murinoglobulin Double-Knockout Mice.

Shemesh CS, Yu RZ, Gaus HJ, Seth PP, Swayze EE, Bennett FC, Geary RS, Henry SP, Wang Y.

Nucleic Acid Ther. 2016 Aug;26(4):223-35. doi: 10.1089/nat.2016.0607. Epub 2016 Mar 31.

PMID:
27031383
8.

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.

PMID:
26914862
9.

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.

PMID:
26299345
10.

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.

PMID:
26011654
11.

Identification of metabolically stable 5'-phosphate analogs that support single-stranded siRNA activity.

Prakash TP, Lima WF, Murray HM, Li W, Kinberger GA, Chappell AE, Gaus H, Seth PP, Bhat B, Crooke ST, Swayze EE.

Nucleic Acids Res. 2015 Mar 31;43(6):2993-3011. doi: 10.1093/nar/gkv162. Epub 2015 Mar 9.

12.

Synthesis, biophysical properties and biological activity of second generation antisense oligonucleotides containing chiral phosphorothioate linkages.

Wan WB, Migawa MT, Vasquez G, Murray HM, Nichols JG, Gaus H, Berdeja A, Lee S, Hart CE, Lima WF, Swayze EE, Seth PP.

Nucleic Acids Res. 2014 Dec 16;42(22):13456-68. doi: 10.1093/nar/gku1115. Epub 2014 Nov 14.

13.

Targeted delivery of antisense oligonucleotides to hepatocytes using triantennary N-acetyl galactosamine improves potency 10-fold in mice.

Prakash TP, Graham MJ, Yu J, Carty R, Low A, Chappell A, Schmidt K, Zhao C, Aghajan M, Murray HF, Riney S, Booten SL, Murray SF, Gaus H, Crosby J, Lima WF, Guo S, Monia BP, Swayze EE, Seth PP.

Nucleic Acids Res. 2014 Jul;42(13):8796-807. doi: 10.1093/nar/gku531. Epub 2014 Jul 3.

14.

Formation of the N(2)-acetyl-2,6-diaminopurine oligonucleotide impurity caused by acetyl capping.

Rodriguez AA, Cedillo I, Mowery BP, Gaus HJ, Krishnamoorthy SS, McPherson AK.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3243-6. doi: 10.1016/j.bmcl.2014.06.025. Epub 2014 Jun 18.

PMID:
24980055
15.

Pharmacology of a central nervous system delivered 2'-O-methoxyethyl-modified survival of motor neuron splicing oligonucleotide in mice and nonhuman primates.

Rigo F, Chun SJ, Norris DA, Hung G, Lee S, Matson J, Fey RA, Gaus H, Hua Y, Grundy JS, Krainer AR, Henry SP, Bennett CF.

J Pharmacol Exp Ther. 2014 Jul;350(1):46-55. doi: 10.1124/jpet.113.212407. Epub 2014 Apr 30.

16.

Single-stranded siRNAs activate RNAi in animals.

Lima WF, Prakash TP, Murray HM, Kinberger GA, Li W, Chappell AE, Li CS, Murray SF, Gaus H, Seth PP, Swayze EE, Crooke ST.

Cell. 2012 Aug 31;150(5):883-94. doi: 10.1016/j.cell.2012.08.014.

17.

Widespread recognition of 5' splice sites by noncanonical base-pairing to U1 snRNA involving bulged nucleotides.

Roca X, Akerman M, Gaus H, Berdeja A, Bennett CF, Krainer AR.

Genes Dev. 2012 May 15;26(10):1098-109. doi: 10.1101/gad.190173.112.

18.

Evaluating free-choice climate education interventions applying propensity score matching.

Gaus H, Mueller CE.

Eval Rev. 2011 Dec;35(6):673-722. doi: 10.1177/0193841X12439703.

PMID:
22473495
19.

Synthesis, improved antisense activity and structural rationale for the divergent RNA affinities of 3'-fluoro hexitol nucleic acid (FHNA and Ara-FHNA) modified oligonucleotides.

Egli M, Pallan PS, Allerson CR, Prakash TP, Berdeja A, Yu J, Lee S, Watt A, Gaus H, Bhat B, Swayze EE, Seth PP.

J Am Chem Soc. 2011 Oct 19;133(41):16642-9. doi: 10.1021/ja207086x. Epub 2011 Sep 22.

20.

In vitro metabolic stabilities and metabolism of 2'-O-(methoxyethyl) partially modified phosphorothioate antisense oligonucleotides in preincubated rat or human whole liver homogenates.

Baek MS, Yu RZ, Gaus H, Grundy JS, Geary RS.

Oligonucleotides. 2010 Dec;20(6):309-16. doi: 10.1089/oli.2010.0252. Epub 2010 Nov 30.

PMID:
21117960
21.

Configuration of the 5'-methyl group modulates the biophysical and biological properties of locked nucleic acid (LNA) oligonucleotides.

Seth PP, Allerson CR, Siwkowski A, Vasquez G, Berdeja A, Migawa MT, Gaus H, Prakash TP, Bhat B, Swayze EE.

J Med Chem. 2010 Dec 9;53(23):8309-18. doi: 10.1021/jm101207e. Epub 2010 Nov 8.

PMID:
21058707
22.

An exocyclic methylene group acts as a bioisostere of the 2'-oxygen atom in LNA.

Seth PP, Allerson CR, Berdeja A, Siwkowski A, Pallan PS, Gaus H, Prakash TP, Watt AT, Egli M, Swayze EE.

J Am Chem Soc. 2010 Oct 27;132(42):14942-50. doi: 10.1021/ja105875e.

23.

Peptide nucleic acids conjugated to short basic peptides show improved pharmacokinetics and antisense activity in adipose tissue.

Wancewicz EV, Maier MA, Siwkowski AM, Albertshofer K, Winger TM, Berdeja A, Gaus H, Vickers TA, Bennett CF, Monia BP, Griffey RH, Nulf CJ, Hu J, Corey DR, Swayze EE, Kinberger GA.

J Med Chem. 2010 May 27;53(10):3919-26. doi: 10.1021/jm901489k.

24.

Synthesis and biophysical evaluation of 2',4'-constrained 2'O-methoxyethyl and 2',4'-constrained 2'O-ethyl nucleic acid analogues.

Seth PP, Vasquez G, Allerson CA, Berdeja A, Gaus H, Kinberger GA, Prakash TP, Migawa MT, Bhat B, Swayze EE.

J Org Chem. 2010 Mar 5;75(5):1569-81. doi: 10.1021/jo902560f.

PMID:
20136157
25.

Antisense oligonucleotides containing conformationally constrained 2',4'-(N-methoxy)aminomethylene and 2',4'-aminooxymethylene and 2'-O,4'-C-aminomethylene bridged nucleoside analogues show improved potency in animal models.

Prakash TP, Siwkowski A, Allerson CR, Migawa MT, Lee S, Gaus HJ, Black C, Seth PP, Swayze EE, Bhat B.

J Med Chem. 2010 Feb 25;53(4):1636-50. doi: 10.1021/jm9013295.

PMID:
20108935
26.

Amphoteric liposomes enable systemic antigen-presenting cell-directed delivery of CD40 antisense and are therapeutically effective in experimental arthritis.

Andreakos E, Rauchhaus U, Stavropoulos A, Endert G, Wendisch V, Benahmed AS, Giaglis S, Karras J, Lee S, Gaus H, Bennett CF, Williams RO, Sideras P, Panzner S.

Arthritis Rheum. 2009 Apr;60(4):994-1005. doi: 10.1002/art.24434.

27.

Human Dicer binds short single-strand and double-strand RNA with high affinity and interacts with different regions of the nucleic acids.

Lima WF, Murray H, Nichols JG, Wu H, Sun H, Prakash TP, Berdeja AR, Gaus HJ, Crooke ST.

J Biol Chem. 2009 Jan 23;284(4):2535-48. doi: 10.1074/jbc.M803748200. Epub 2008 Nov 18.

28.

Design, synthesis and evaluation of constrained methoxyethyl (cMOE) and constrained ethyl (cEt) nucleoside analogs.

Seth PP, Siwkowski A, Allerson CR, Vasquez G, Lee S, Prakash TP, Kinberger G, Migawa MT, Gaus H, Bhat B, Swayze EE.

Nucleic Acids Symp Ser (Oxf). 2008;(52):553-4. doi: 10.1093/nass/nrn280.

PMID:
18776499
29.

Cross-species pharmacokinetic comparison from mouse to man of a second-generation antisense oligonucleotide, ISIS 301012, targeting human apolipoprotein B-100.

Yu RZ, Kim TW, Hong A, Watanabe TA, Gaus HJ, Geary RS.

Drug Metab Dispos. 2007 Mar;35(3):460-8. Epub 2006 Dec 15.

PMID:
17172312
30.
31.

Formation of modified cytosine residues in the presence of depurinated DNA.

Rentel C, Wang X, Batt M, Kurata C, Oliver J, Gaus H, Krotz AH, McArdle JV, Capaldi DC.

J Org Chem. 2005 Sep 30;70(20):7841-5.

PMID:
16277303
32.

Characterization of high molecular weight impurities in synthetic phosphorothioate oligonucleotides.

Kurata C, Bradley K, Gaus H, Luu N, Cedillo I, Ravikumar VT, Van Sooy K, McArdle JV, Capaldi DC.

Bioorg Med Chem Lett. 2006 Feb;16(3):607-14. Epub 2005 Nov 7.

PMID:
16274991
33.

Trichloroacetaldehyde modified oligonucleotides.

Gaus H, Olsen P, Sooy KV, Rentel C, Turney B, Walker KL, McArdle JV, Capaldi DC.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4118-24.

PMID:
16002284
34.

Formation of oligonucleotide adducts in pharmaceutical formulations.

Krotz AH, Gaus H, Hardee GE.

Pharm Dev Technol. 2005;10(2):283-90.

PMID:
15926677
35.

Formation of 4,4'-dimethoxytrityl-C-phosphonate oligonucleotides.

Capaldi DC, Gaus HJ, Carty RL, Moore MN, Turney BJ, Decottignies SD, McArdle JV, Scozzari AN, Ravikumar VT, Krotz AH.

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4683-90.

PMID:
15324888
36.

Solution stability and degradation pathway of deoxyribonucleoside phosphoramidites in acetonitrile.

Krotz AH, Rentel C, Gorman D, Olsen P, Gaus HJ, McArdle JV, Scozzari AN.

Nucleosides Nucleotides Nucleic Acids. 2004 May;23(5):767-75.

PMID:
15281365
37.

Synthesis and characterization of oligonucleotides containing conformationally constrained bicyclo[3.1.0]hexane pseudosugar analogs.

Maier MA, Choi Y, Gaus H, Barchi JJ Jr, Marquez VE, Manoharan M.

Nucleic Acids Res. 2004 Jul 9;32(12):3642-50. Print 2004.

38.

Alternative approaches to infrared multiphoton dissociation in an external ion reservoir.

Hofstadler SA, Drader JJ, Gaus H, Hannis JC, Sannes-Lowery KA.

J Am Soc Mass Spectrom. 2003 Dec;14(12):1413-23.

39.

Preparation of oligonucleotides without aldehyde abasic sites.

Krotz AH, Gaus H, Ravikumar VT, Cole DL.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1863-7.

PMID:
11459648
40.

Hepatic distribution of a phosphorothioate oligodeoxynucleotide within rodents following intravenous administration.

Graham MJ, Crooke ST, Lemonidis KM, Gaus HJ, Templin MV, Crooke RM.

Biochem Pharmacol. 2001 Aug 1;62(3):297-306.

PMID:
11434902
41.

Monitoring solution-phase combinatorial library synthesis by capillary electrophoresis.

Gaus HJ, Kung PP, Brooks D, Cook PD, Cummins LL.

Biotechnol Bioeng. 1998-1999;61(3):169-77.

PMID:
10397804
42.

Characterization of oligonucleotide metabolism in vivo via liquid chromatography/electrospray tandem mass spectrometry with a quadrupole ion trap mass spectrometer.

Griffey RH, Greig MJ, Gaus HJ, Liu K, Monteith D, Winniman M, Cummins LL.

J Mass Spectrom. 1997 Mar;32(3):305-13.

PMID:
9075339
43.

On-line HPLC electrospray mass spectrometry of phosphorothioate oligonucleotide metabolites.

Gaus HJ, Owens SR, Winniman M, Cooper S, Cummins LL.

Anal Chem. 1997 Feb 1;69(3):313-9.

PMID:
9030048
44.

Negative ionization micro electrospray mass spectrometry of oligonucleotides and their complexes.

Greig MJ, Gaus HJ, Griffey RH.

Rapid Commun Mass Spectrom. 1996;10(1):47-50.

PMID:
8563016
45.

Superantigen-reactive T cells that display an anergic phenotype in vitro appear functional in vivo.

Heeg K, Gaus H, Griese D, Bendigs S, Miethke T, Wagner H.

Int Immunol. 1995 Jan;7(1):105-14.

PMID:
7718507
46.

Analysis of double-stranded oligonucleotides by electrospray mass spectrometry.

Bayer E, Bauer T, Schmeer K, Bleicher K, Maier M, Gaus HJ.

Anal Chem. 1994 Nov 15;66(22):3858-63.

PMID:
7810895
47.
48.
49.

Superantigen mediated shock: a cytokine release syndrome.

Miethke T, Wahl C, Regele D, Gaus H, Heeg K, Wagner H.

Immunobiology. 1993 Nov;189(3-4):270-84. Review.

PMID:
8125513
50.

Optimization of capillary electrophoresis of mixtures of basic peptides and comparison with HPLC.

Gaus HJ, Beck-Sickinger AG, Bayer E.

Anal Chem. 1993 May 15;65(10):1399-405.

PMID:
8517549

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