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Towards next generation antisense oligonucleotides: mesylphosphoramidate modification improves therapeutic index and duration of effect of gapmer antisense oligonucleotides

Nucleic acids research, 2021-09, Vol.49 (16), p.9026-9041

2021

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Chemical modification of PS-ASO therapeutics reduces cellular protein-binding and improves the therapeutic index

Nature biotechnology, 2019-06, Vol.37 (6), p.640-650

2019

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Translation efficiency of mRNAs is increased by antisense oligonucleotides targeting upstream open reading frames

Nature biotechnology, 2016-08, Vol.34 (8), p.875-880

2016

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Site-specific incorporation of 5'-methyl DNA enhances the therapeutic profile of gapmer ASOs

Nucleic acids research, 2021-02, Vol.49 (4), p.1828-1839

2021

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Understanding the effect of controlling phosphorothioate chirality in the DNA gap on the potency and safety of gapmer antisense oligonucleotides

Nucleic acids research, 2020-02, Vol.48 (4), p.1691-1700

2020

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

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2718-2733

2016

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

Nucleic acids research, 2014-12, Vol.42 (22), p.13456-13468

2014

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

Bioconjugate chemistry, 2015-08, Vol.26 (8), p.1451-1455

2015

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Antisense oligonucleotides containing locked nucleic acid improve potency but cause significant hepatotoxicity in animals

Nucleic acids research, 2007-01, Vol.35 (2), p.687-700

2007

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Evaluation of Phosphorus and Non-Phosphorus Neutral Oligonucleotide Backbones for Enhancing Therapeutic Index of Gapmer Antisense Oligonucleotides

Nucleic acid therapeutics, 2022-02, Vol.32 (1), p.40-50

2022

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Site-specific replacement of phosphorothioate with alkyl phosphonate linkages enhances the therapeutic profile of gapmer ASOs by modulating interactions with cellular proteins

Nucleic acids research, 2019-06, Vol.47 (11), p.5465-5479

2019

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Alternative Syntheses of (S)‑cEt-BNA: A Key Constrained Nucleoside Component of Bioactive Antisense Gapmer Sequences

Journal of organic chemistry, 2014-12, Vol.79 (23), p.11651-11660

2014

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

Molecular therapy. Nucleic acids, 2016, Vol.5 (5), p.e319, Article e319

2016

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Antisense oligonucleotides targeting translation inhibitory elements in 5' UTRs can selectively increase protein levels

Nucleic acids research, 2017-09, Vol.45 (16), p.9528-9546

2017

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

Bioorganic & medicinal chemistry letters, 2015-10, Vol.25 (19), p.4127-4130

2015

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

Bioorganic & medicinal chemistry letters, 2016-05, Vol.26 (9), p.2194-2197

2016

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Interaction of ASOs with PC4 Is Highly Influenced by the Cellular Environment and ASO Chemistry

Journal of the American Chemical Society, 2020-05, Vol.142 (21), p.9661-9674, Article jacs.0c01808

2020

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High-resolution visualization and quantification of nucleic acid-based therapeutics in cells and tissues using Nanoscale secondary ion mass spectrometry (NanoSIMS)

Nucleic acids research, 2021-01, Vol.49 (1), p.1-14

2021

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Configuration of the 5′-Methyl Group Modulates the Biophysical and Biological Properties of Locked Nucleic Acid (LNA) Oligonucleotides

Journal of medicinal chemistry, 2010-12, Vol.53 (23), p.8309-8318

2010

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Systematic Investigation of Tether Length and Phosphorus Configuration in Backbone Constrained Macrocyclic Nucleic Acids to Modulate Binding Kinetics for RNA

Journal of organic chemistry, 2023-03, Vol.88 (6), p.3599-3614

2023

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Backbone Hydrocarbon-Constrained Nucleic Acids Modulate Hybridization Kinetics for RNA

Journal of the American Chemical Society, 2022-02, Vol.144 (4), p.1941-1950

2022

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Synthesis and Biophysical Evaluation of 2′,4′-Constrained 2′O-Methoxyethyl and 2′,4′-Constrained 2′O-Ethyl Nucleic Acid Analogues

Journal of organic chemistry, 2010-03, Vol.75 (5), p.1569-1581

2010

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Human RNase H1 Discriminates between Subtle Variations in the Structure of the Heteroduplex Substrate

Molecular pharmacology, 2007-01, Vol.71 (1), p.83-91

2007

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Synthesis and Biophysical Properties of Constrained d‑Altritol Nucleic Acids (cANA)

Organic letters, 2013-09, Vol.15 (17), p.4316-4319

2013

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The Positional Influence of the Helical Geometry of the Heteroduplex Substrate on Human RNase H1 Catalysis

Molecular pharmacology, 2007-01, Vol.71 (1), p.73-82

2007

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Towards next generation antisense oligonucleotides: mesylphosphoramidate modification improves therapeutic index and duration of effect of gapmer antisense oligonucleotides

Chemical modification of PS-ASO therapeutics reduces cellular protein-binding and improves the therapeutic index

Translation efficiency of mRNAs is increased by antisense oligonucleotides targeting upstream open reading frames

Site-specific incorporation of 5'-methyl DNA enhances the therapeutic profile of gapmer ASOs

Understanding the effect of controlling phosphorothioate chirality in the DNA gap on the potency and safety of gapmer antisense oligonucleotides

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

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

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

Antisense oligonucleotides containing locked nucleic acid improve potency but cause significant hepatotoxicity in animals

Evaluation of Phosphorus and Non-Phosphorus Neutral Oligonucleotide Backbones for Enhancing Therapeutic Index of Gapmer Antisense Oligonucleotides

Site-specific replacement of phosphorothioate with alkyl phosphonate linkages enhances the therapeutic profile of gapmer ASOs by modulating interactions with cellular proteins

Alternative Syntheses of (S)‑cEt-BNA: A Key Constrained Nucleoside Component of Bioactive Antisense Gapmer Sequences

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

Antisense oligonucleotides targeting translation inhibitory elements in 5' UTRs can selectively increase protein levels

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

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

Interaction of ASOs with PC4 Is Highly Influenced by the Cellular Environment and ASO Chemistry

High-resolution visualization and quantification of nucleic acid-based therapeutics in cells and tissues using Nanoscale secondary ion mass spectrometry (NanoSIMS)

Configuration of the 5′-Methyl Group Modulates the Biophysical and Biological Properties of Locked Nucleic Acid (LNA) Oligonucleotides

Systematic Investigation of Tether Length and Phosphorus Configuration in Backbone Constrained Macrocyclic Nucleic Acids to Modulate Binding Kinetics for RNA

Backbone Hydrocarbon-Constrained Nucleic Acids Modulate Hybridization Kinetics for RNA

Synthesis and Biophysical Evaluation of 2′,4′-Constrained 2′O-Methoxyethyl and 2′,4′-Constrained 2′O-Ethyl Nucleic Acid Analogues

Human RNase H1 Discriminates between Subtle Variations in the Structure of the Heteroduplex Substrate

Synthesis and Biophysical Properties of Constrained d‑Altritol Nucleic Acids (cANA)

The Positional Influence of the Helical Geometry of the Heteroduplex Substrate on Human RNase H1 Catalysis

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