Gaus HJ - Search Results

1

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. Shemesh CS, et al. Among authors: gaus hj. Nucleic Acid Ther. 2016 Aug;26(4):223-35. doi: 10.1089/nat.2016.0607. Epub 2016 Mar 31. Nucleic Acid Ther. 2016. PMID: 27031383

2

Improving RNA interference in mammalian cells by 4'-thio-modified small interfering RNA (siRNA): effect on siRNA activity and nuclease stability when used in combination with 2'-O-alkyl modifications.

Dande P, Prakash TP, Sioufi N, Gaus H, Jarres R, Berdeja A, Swayze EE, Griffey RH, Bhat B. Dande P, et al. J Med Chem. 2006 Mar 9;49(5):1624-34. doi: 10.1021/jm050822c. J Med Chem. 2006. PMID: 16509579

3

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. Yu RZ, et al. Among authors: gaus hj. Drug Metab Dispos. 2007 Mar;35(3):460-8. doi: 10.1124/dmd.106.012401. Epub 2006 Dec 15. Drug Metab Dispos. 2007. PMID: 17172312 Clinical Trial.

4

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. Seth PP, et al. Nucleic Acids Symp Ser (Oxf). 2008;(52):553-4. doi: 10.1093/nass/nrn280. Nucleic Acids Symp Ser (Oxf). 2008. PMID: 18776499

5

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. Prakash TP, et al. Among authors: gaus hj. J Med Chem. 2010 Feb 25;53(4):1636-50. doi: 10.1021/jm9013295. J Med Chem. 2010. PMID: 20108935

6

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. Seth PP, et al. J Org Chem. 2010 Mar 5;75(5):1569-81. doi: 10.1021/jo902560f. J Org Chem. 2010. PMID: 20136157

7

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. Wancewicz EV, et al. J Med Chem. 2010 May 27;53(10):3919-26. doi: 10.1021/jm901489k. J Med Chem. 2010. PMID: 20420385 Free PMC article.

8

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. Seth PP, et al. J Am Chem Soc. 2010 Oct 27;132(42):14942-50. doi: 10.1021/ja105875e. J Am Chem Soc. 2010. PMID: 20886816 Free PMC article.

9

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. Seth PP, et al. J Med Chem. 2010 Dec 9;53(23):8309-18. doi: 10.1021/jm101207e. Epub 2010 Nov 8. J Med Chem. 2010. PMID: 21058707

10

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. Baek MS, et al. Oligonucleotides. 2010 Dec;20(6):309-16. doi: 10.1089/oli.2010.0252. Epub 2010 Nov 30. Oligonucleotides. 2010. PMID: 21117960

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