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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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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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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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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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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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Antibacterial Aminoglycosides with a Modified Mode of Binding to the Ribosomal-RNA Decoding Site

Angewandte Chemie International Edition, 2004-12, Vol.43 (48), p.6735-6738

2004

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Structure-based design, synthesis and A-site rRNA co-crystal complexes of novel amphiphilic aminoglycoside antibiotics with new binding modes: A synergistic hydrophobic effect against resistant bacteria

Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.7097-7101

2010

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Antibacterial Aminoglycosides with a Modified Mode of Binding to the Ribosomal-RNA Decoding Site

Angewandte Chemie International Edition, 2007-04, Vol.46 (17), p.2971-2971

2007

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Design, Synthesis And Evaluation Of Constrained Methoxyethyl (cMOE) and Constrained Ethyl (cEt) Nucleoside Analogs

Nucleic Acids Symposium Series, 2008-09, Vol.52 (1), p.553-554

2008

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Aryl urea analogs with broad-spectrum antibacterial activity

Bioorganic & medicinal chemistry letters, 2004-11, Vol.14 (22), p.5569-5572

2004

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Synthesis and Unusual Chemical Reactivity of Certain Novel 4,5-Disubstituted 7-Benzylpyrrolo[2,3-d][1,2,3]triazines

Journal of organic chemistry, 2001-07, Vol.66 (14), p.4776-4782

2001

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A Solid-Phase Synthesis of N,N‘-Disubstituted Ureas and Perhydroimidazo[1,5-a]pyrazines via the Curtius Rearrangement

Organic letters, 2000-10, Vol.2 (21), p.3309-3311

2000

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An Efficient Synthesis of Gougerotin and Related Analogues Using Solid- and Solution-Phase Methodology

Organic letters, 2005-08, Vol.7 (16), p.3429-3432

2005

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The synthesis and 16S A-site rRNA recognition of carbohydrate-free aminoglycosides

Bioorganic & medicinal chemistry letters, 2005-11, Vol.15 (22), p.4919-4922

2005

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Synthesis and Biological Activity of 5-Fluorotubercidin

Nucleosides, nucleotides & nucleic acids, 2004-01, Vol.23 (1-2), p.161-170

2004

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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

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

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

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

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

Antibacterial Aminoglycosides with a Modified Mode of Binding to the Ribosomal-RNA Decoding Site

Structure-based design, synthesis and A-site rRNA co-crystal complexes of novel amphiphilic aminoglycoside antibiotics with new binding modes: A synergistic hydrophobic effect against resistant bacteria

Antibacterial Aminoglycosides with a Modified Mode of Binding to the Ribosomal-RNA Decoding Site

Design, Synthesis And Evaluation Of Constrained Methoxyethyl (cMOE) and Constrained Ethyl (cEt) Nucleoside Analogs

Aryl urea analogs with broad-spectrum antibacterial activity

Synthesis and Unusual Chemical Reactivity of Certain Novel 4,5-Disubstituted 7-Benzylpyrrolo[2,3-d][1,2,3]triazines

A Solid-Phase Synthesis of N,N‘-Disubstituted Ureas and Perhydroimidazo[1,5-a]pyrazines via the Curtius Rearrangement

An Efficient Synthesis of Gougerotin and Related Analogues Using Solid- and Solution-Phase Methodology

The synthesis and 16S A-site rRNA recognition of carbohydrate-free aminoglycosides

Synthesis and Biological Activity of 5-Fluorotubercidin

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