ArticleNucleic acids research2013
Design, synthesis and biological evaluation of novel antagonist compounds of Toll-like receptors 7, 8 and 9.
Article in Nucleic acids research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 65 citations in OpenAlex.
- TLR7 in systemic lupus erythematosus: genetics and emerging therapies.Nature reviews. Rheumatology · 2026Review
- Integrated docking-molecular dynamics, ADME-toxicity profiling, and transcriptomic validation identify oroxylin a as a TLR7-targeting flavonoid candidate in systemic lupus erythematosus.Frontiers in chemistry · 2026Article
- Novel Immune Response Evasion Strategy to Redose Adeno-associated Viral Vectors and Prolong Survival in Surfactant Protein-B-Deficient Mice.American journal of respiratory cell and molecular biology · 2025Article
- Dexamethasone loaded DNA scavenger nanogel for systemic lupus erythematosus treatment.Bioactive materials · 2025Article
- A review of the complex interplay between chemoresistance and lncRNAs in lung cancer.Journal of translational medicine · 2024Review
- 2'-Nucleic acid therapeutics · 2022Article
- Phytochemicals targeting Toll-like receptors 4 (TLR4) in inflammatory bowel disease.Chinese medicine · 2022Review
- Nucleic acid-sensing toll-like receptors: Important players in Sjögren's syndrome.Frontiers in immunology · 2022Review
- Targeting Toll-like Receptor (TLR) Pathways in Inflammatory Arthritis: Two Better Than One?Biomolecules · 2021Review
- Thermostability, Tunability, and Tenacity of RNA as Rubbery Anionic Polymeric Materials in Nanotechnology and Nanomedicine-Specific Cancer Targeting with Undetectable Toxicity.Chemical reviews · 2021Review
- The Evolution of Antisense Oligonucleotide Chemistry-A Personal Journey.Biomedicines · 2021Review
- LncRNAs in Cancer: From garbage to Junk.Cancers · 2020Review
- Advances in oligonucleotide drug delivery.Nature reviews. Drug discovery · 2020Review
- Macrophage polarization in innate immune responses contributing to pathogenesis of chronic kidney disease.BMC nephrology · 2020Review
- Article
- Progressive Skeletal Muscle Atrophy in Muscular Dystrophies: A Role for Toll-like Receptor-Signaling in Disease Pathogenesis.International journal of molecular sciences · 2020Review
- Phosphorothioate modified oligonucleotide-protein interactions.Nucleic acids research · 2020Article
- Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes.European journal of medicinal chemistry · 2020Review
- A Dual TLR7/TLR9 Inhibitor HJ901 Inhibits ABC-DLBCL Expressing the MyD88 L265P Mutation.Frontiers in cell and developmental biology · 2020Article
- Receptor targeting drug delivery strategies and prospects in the treatment of rheumatoid arthritis.Research in pharmaceutical sciences · 2019Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oligonucleotides containing an immune-stimulatory motif and an immune-regulatory motif act as antagonists of Toll-like receptor (TLR)7 and TLR9. In the present study, we designed and synthesized oligonucleotide-based antagonists of TLR7, 8 and 9 containing a 7-deaza-dG or arabino-G modification in the immune-stimulatory motif and 2'-O-methylribonucleotides as the immune-regulatory motif. We evaluated the biological properties of these novel synthetic oligoribonucleotides as antagonists of TLRs 7, 8 and 9 in murine and human cell-based assays and in vivo in mice and non-human primates. In HEK293, mouse and human cell-based assays, the antagonist compounds inhibited signaling pathways and production of a broad range of cytokines, including tumour necrosis factor alpha (TNF-α), interleukin (IL)-12, IL-6, interferon (IFN)-α, IL-1β and interferon gamma-induced protein (IP)-10, mediated by TLR7, 8 and 9. In vivo in mice, the antagonist compounds inhibited TLR7- and TLR9-mediated cytokine induction in a dose- and time-dependent fashion. Peripheral blood mononuclear cells (PBMCs) obtained from antagonist compound-treated monkeys secreted lower levels of TLR7-, 8- and 9-mediated cytokines than did PBMCs taken before antagonist administration. The antagonist compounds described herein provide novel agents for the potential treatment of autoimmune and inflammatory diseases.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.