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Pharmacokinetics of Antisense Oligonucleotides

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Evaluation of the safety, tolerability and pharmacokinetics of ALN-RSV01, a novel RNAi antiviral therapeutic directed against respiratory syncytial virus (RSV)

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Inhibition of human immunodeficiency virus replication by antisense oligodeoxynucleotides.

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Mixed-backbone oligonucleotides as second generation antisense oligonucleotides: <i>In vitro</i> and <i>in vivo</i>  studies

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Inhibition of human immunodeficiency virus in early infected and chronically infected cells by antisense oligodeoxynucleotides and their phosphorothioate analogues.

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RNAi-Based Treatment for Neovascular Age-Related Macular Degeneration by Sirna-027

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Importance of nucleotide sequence and chemical modifications of antisense oligonucleotides

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Small interfering RNA-induced TLR3 activation inhibits blood and lymphatic vessel growth

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Antisense therapeutics: is it as simple as complementary base recognition?

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Absorption, tissue distribution and in vivo stability in rats of a hybrid antisense oligonucleotide following oral administration

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Inhibition of acquired immunodeficiency syndrome virus by oligodeoxynucleoside methylphosphonates.

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Antisense and siRNA as agonists of Toll-like receptors

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Pharmacokinetics and tissue distribution in rats of an oligodeoxynucleotide phosphorothioate (GEM 91) developed as a therapeutic agent for human immunodeficiency virus type-1

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Similar behaviour of single-strand and double-strand siRNAs suggests they act through a common RNAi pathway

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Immune stimulation by an antisense oligomer complementary to the rev gene of HIV-1

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The Therapeutic Potential of Ribozymes

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Effects on RNA Interference in Gene Expression (RNAi) in Cultured Mammalian Cells of Mismatches and the Introduction of Chemical Modifications at the 3′-Ends of siRNAs

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Pattern and Kinetics of Cytokine Production Following Administration of Phosphorothioate Oligonucleotides in Mice

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In vivo stability, disposition and metabolism of a “hybrid” oligonucleotide phosphorothioate in rats

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Conjugation of Ligands at the 5‘-End of CpG DNA Affects Immunostimulatory Activity

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Self-stabilized antisense oligodeoxynucleotide phosphorothioates: properties and anti-HIV activity

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Mixed Backbone Oligonucleotides: Improvement in Oligonucleotide-induced Toxicity In Vivo

Agrawal, S., & Zhao, Q. (1998) · Antisense and Nucleic Acid Drug Development · doi:10.1089/oli.1.1998.8.135 · Cited by 80 · see citing works

'Immunomers'--novel 3'-3'-linked CpG oligodeoxyribonucleotides as potent immunomodulatory agents

Yu, D. S. (2002) · Nucleic Acids Research · doi:10.1093/nar/gkf582 · Cited by 80 · see citing works

Pharmacokinetics, Biodistribution, and Stability of Capped Oligodeoxynucleotide Phosphorothioates in Mice

Temsamani, J., Tang, J. Y., Padmapriya, A. A., Kubert, M., & Agrawal, S. (1993) · Antisense Research and Development · doi:10.1089/ard.1993.3.277 · Cited by 75 · see citing works

Accessible 5′-end of CpG-containing Phosphorothioate Oligodeoxynucleotides is essential for immunostimulatory activity

Yu, D. S., Zhao, Q., Kandimalla, E. R., & Agrawal, S. (2000) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(00)00537-0 · Cited by 72 · see citing works

Modulation of malignant B cell activation and apoptosis by bcl-2 antisense ODN and immunostimulatory CpG ODN

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Study of antisense oligonucleotide phosphorothioates containing segments of oligodeoxynucleotides and 2′-o- methyloligoribonucleotides

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Small Interfering RNAs Induce Target-Independent Inhibition of Tumor Growth and Vasculature Remodeling in a Mouse Model of Hepatocellular Carcinoma

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Pharmacokinetics and tissue disposition of a chimeric oligodeoxynucleoside phosphorothioate in rats after intravenous administration.

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In vivo stability and disposition of a self-stabilized oligodeoxynucleotide phosphorothioate in rats

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Cellular Distribution of Phosphorothioate Oligonucleotide Following Intravenous Administration in Mice

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Pharmacokinetics and Metabolism of an Oligodeoxynucleotide Phosphorothioate (GEM91®) in Cynomolgus Monkeys Following Intravenous Infusion

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Administration of a Phosphorothioate Oligonucleotide Antisense to Murine Endogenous Retroviral MCF env Causes Immune Effects in Vivo in a Sequence-Specific Manner

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In vitro binding of single‐stranded RNA by human Dicer

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Toll-like Receptor 7 Selective Synthetic Oligoribonucleotide Agonists: Synthesis and Structure−Activity Relationship Studies

Lan, T., Dai, M., Wang, D., Zhu, F., Kandimalla, E. R., & Agrawal, S. (2009) · Journal of Medicinal Chemistry · doi:10.1021/jm901145s · Cited by 27 · see citing works

Novel enzymatic and immunological responses to oligonucleotides

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Non-specific antiviral activity of antisense molecules targeted to the E1 region of human papillomavirus

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Capped Oligodeoxynucleotide Phosphorothioates.

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Biodistribution and Metabolism of a Mixed Backbone Oligonucleotide (GEM 231) Following Single and Multiple Dose Administration in Mice

Rusckowski, M., QU, T., Roskey, A., & Agrawal, S. (2000) · Antisense and Nucleic Acid Drug Development · doi:10.1089/oli.1.2000.10.333 · Cited by 20 · see citing works

Synthesis and Anti‐HIV Activity of Oligoribonucleotides and Their Phosphorothioate Analogs

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3′-3′-linked oligonucleotides: Synthesis and stability studies

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Effects of phosphorothioate oligodeoxyribonucleotide and oligoribonucleotides on human complement and coagulation

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Advances in antisense efficacy and delivery

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Synthesis of oligodeoxynucleoside methylphosphonothioates

Padmapriya, A. A., & Agrawal, S. (1993) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/s0960-894x(01)81270-1 · Cited by 14 · see citing works

Synthesis, gene-silencing activity and nuclease resistance of 3′–3′-linked double short hairpin RNA

Masuda, H., Watanabe, N., Naruoka, H., Nagata, S., Takagaki, K., Wada, T., & Yano, J. (2010) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2010.10.001 · Cited by 10 · see citing works

Repression of Human Thymidylate Synthase mRNA Translation by Antisense 2′-O-Methyl Oligoribonucleotides

Schmitz, J. C., Agrawal, S., & Chu, E. (1998) · Antisense and Nucleic Acid Drug Development · doi:10.1089/oli.1.1998.8.371 · Cited by 6 · see citing works

The chemical evolution of oligonucleotide therapies of clinical utility

Khvorova, A., & Watts, J. K. (2017) · Nature Biotechnology · doi:10.1038/nbt.3765 · Cited by 1,216 · see citing works

A divalent siRNA chemical scaffold for potent and sustained modulation of gene expression throughout the central nervous system

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Myeloid Differentiation Primary Response Protein 88 (MyD88): The Central Hub of TLR/IL-1R Signaling

Chen, L., Zheng, L., Chen, P., & Liang, G. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00884 · Cited by 153 · see citing works

Inhibition of 14q32 MicroRNAs miR-329, miR-487b, miR-494, and miR-495 Increases Neovascularization and Blood Flow Recovery After Ischemia

Welten, S. M. J., Bastiaansen, A. J. N. M., de Jong, R. C. M., de Vries, M. R., Peters, E. A. B., Boonstra, M. C., Sheikh, S. P., Monica, N. L., Kandimalla, E. R., Quax, P. H. A., et al. (2014) · Circulation Research · doi:10.1161/circresaha.114.304747 · Cited by 144 · see citing works

Inhibition of 14q32 microRNA miR-495 reduces lesion formation, intimal hyperplasia and plasma cholesterol levels in experimental restenosis

Welten, S. M. J., de Jong, R. C. M., Wezel, A., de Vries, M. R., Boonstra, M. C., Parma, L., Jukema, J. W., van der Sluis, T. C., Arens, R., Bot, I., et al. (2017) · Atherosclerosis · doi:10.1016/j.atherosclerosis.2017.04.011 · Cited by 36 · see citing works

Enhancing antisense efficacy with multimers and multi-targeting oligonucleotides (MTOs) using cleavable linkers

Subramanian, R. R., Wysk, M., Ogilvie, K. M., Bhat, A., Kuang, B., Rockel, T. D., Weber, M., Uhlmann, E., & Krieg, A. Μ. (2015) · Nucleic Acids Research · doi:10.1093/nar/gkv992 · Cited by 25 · see citing works

The Evolution of Antisense Oligonucleotide Chemistry—A Personal Journey

Agrawal, S. (2021) · Biomedicines · doi:10.3390/biomedicines9050503 · Cited by 21 · see citing works

Inhibition of Mef2a Enhances Neovascularization via Post-transcriptional Regulation of 14q32 MicroRNAs miR-329 and miR-494

Welten, S. M. J., de Vries, M. R., Peters, E. A. B., Agrawal, S., Quax, P. H. A., & Nossent, A. Y. (2017) · Molecular Therapy — Nucleic Acids · doi:10.1016/j.omtn.2017.03.003 · Cited by 16 · see citing works

Evaluation of DNA segments in 2′-modified RNA sequences in designing efficient splice switching antisense oligonucleotides

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Investigation of Sequence‐Penetration Relationships of Antisense Oligonucleotides

Batistatou, N., & Kritzer, J. A. (2023) · ChemBioChem · doi:10.1002/cbic.202300009 · Cited by 12 · see citing works

Chemical Modifications and Design Influence the Potency of Huntingtin Anti-Gene Oligonucleotides

Saher, O., Zaghloul, E. M., Umek, T., Hagey, D. W., Mozafari, N., Danielsen, M. B., Gouda, A. S., Lundin, K. E., Jørgensen, P. T., Wengel, J., et al. (2023) · Nucleic Acid Therapeutics · doi:10.1089/nat.2022.0046 · Cited by 10 · see citing works

History and Development of Nucleotide Analogues in Nucleic Acids Drugs

Agrawal, S., & Gait, M. J. (2019) · Royal Society of Chemistry eBooks · doi:10.1039/9781788015714-00001 · Cited by 10 · see citing works

The Medicinal Chemistry of Antisense Oligonucleotides

Watts, J. K. (2018) · Wiley eBooks · doi:10.1002/9781119070153.ch2 · Cited by 8 · see citing works

Considerations for Creating the Next Generation of RNA Therapeutics: Oligonucleotide Chemistry and Innate Immune Responses to Nucleic Acids

Agrawal, S. (2024) · Nucleic Acid Therapeutics · doi:10.1089/nat.2024.29009.sud · Cited by 4 · see citing works

The role of MyD88 in the nervous system: Neuronal functions, implications in neurological diseases, and therapeutic potential

Pan, H.-L., Ge, J.-Y., Zhang, Z.-A., Xu, J., Wu, J., Ju, Y., Zhang, X.-Y., Jiang, Z.-J., Chen, Y., Xu, Y., et al. (2026) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2026.109016 · Cited by 3 · see citing works

Design, synthesis and anti-influenza virus activities of terminal modified antisense oligonucleotides

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A novel dual lock method for down-regulation of genes, in which a target mRNA is captured at 2 independent positions by linked locked nucleic acid antisense oligonucleotides

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Transient Cyclic Structured Oligonucleotide Designs for Therapeutic Applications

Agrawal, S. (2026) · Current Protocols · doi:10.1002/cpz1.70319 · Cited by 1 · see citing works

Nucleotides and nucleic acids; oligo‐ and polynucleotides

Loakes, D. (2013) · Royal Society of Chemistry eBooks · doi:10.1039/9781849737708-00285 · Cited by 1 · see citing works

Application of Antisense Technology in Medicine

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Oligonucleotide Therapeutics

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Silencing of Gene Expression by Gymnotic Delivery of Antisense Oligonucleotides

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