ArticleJournal of medicinal chemistry2012
Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
28 citing papers in PubMed.
- Review
- Vaccine adjuvants for infectious disease in the clinic.Bioengineering & translational medicine · 2024Review
- Theranostic Small-Molecule Prodrug Conjugates for Targeted Delivery and Controlled Release of Toll-like Receptor 7 Agonists.International journal of molecular sciences · 2022Article
- Integration of Ligand-Based and Structure-Based Methods for the Design of Small-Molecule TLR7 Antagonists.Molecules (Basel, Switzerland) · 2022Article
- A comprehensive review of BBV152 vaccine development, effectiveness, safety, challenges, and prospects.Frontiers in immunology · 2022Review
- Evolution of Toll-like receptor 7/8 agonist therapeutics and their delivery approaches: From antiviral formulations to vaccine adjuvants.Advanced drug delivery reviews · 2021Review
- Structural evolution of toll-like receptor 7/8 agonists from imidazoquinolines to imidazoles.RSC medicinal chemistry · 2021Review
- Th1 skewed immune response of whole virion inactivated SARS CoV 2 vaccine and its safety evaluation.iScience · 2021Article
- Receptor-Ligand Kinetics Influence the Mechanism of Action of Covalently Linked TLR Ligands.ACS chemical biology · 2021Article
- Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes.European journal of medicinal chemistry · 2020Review
- Transcriptomal signatures of vaccine adjuvants and accessory immunostimulation of sentinel cells by toll-like receptor 2/6 agonists.Human vaccines & immunotherapeutics · 2018Article
- Toll-like Receptor Agonist Conjugation: A Chemical Perspective.Bioconjugate chemistry · 2018Review
- Bioconjugation of Small Molecules to RNA Impedes Its Recognition by Toll-Like Receptor 7.Frontiers in immunology · 2017Article
- Immune Response Modulation of Conjugated Agonists with Changing Linker Length.ACS chemical biology · 2016Article
- Beyond antigens and adjuvants: formulating future vaccines.The Journal of clinical investigation · 2016Review
- Identification of Adjuvantic Activity of Amphotericin B in a Novel, Multiplexed, Poly-TLR/NLR High-Throughput Screen.PloS one · 2016Article
- Modulation of Innate Immune ResponsesACS central science · 2015Article
- Structure-Based Design of Human TLR8-Specific Agonists with Augmented Potency and Adjuvanticity.Journal of medicinal chemistry · 2015Article
- Facile syntheses of functionalized toll-like receptor 7 agonists.Tetrahedron letters · 2015Article
- Human Toll-like receptor 8-selective agonistic activities in 1-alkyl-1H-benzimidazol-2-amines.Journal of medicinal chemistry · 2014Article
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
Toll-like receptors (TLRs) are pattern recognition receptors that recognize specific molecular patterns present in molecules that are broadly shared by pathogens but are structurally distinct from host molecules. The TLR7-agonistic imidazoquinolines are of interest as vaccine adjuvants given their ability to induce pronounced Th1-skewed humoral responses. Minor modifications on the imidazoquinoline scaffold result in TLR7-antagonistic compounds which may be of value in addressing innate immune activation-driven immune exhaustion observed in HIV. We describe the syntheses and evaluation of TLR7 and TLR8 modulatory activities of dimeric constructs of imidazoquinoline linked at the C2, C4, C8, and N(1)-aryl positions. Dimers linked at the C4, C8, and N(1)-aryl positions were agonistic at TLR7; only the N(1)-aryl dimer with a 12-carbon linker was dual TLR7/8 agonistic. Dimers linked at C2 position showed antagonistic activities at TLR7 and TLR8; the C2 dimer with a propylene spacer was maximally antagonistic at both TLR7 and TLR8.
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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.