Targeting Toll-like receptors: emerging therapeutics?
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Updated: Jun 14, 2026

Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling
Published on: July 26, 2017
Elizabeth J Hennessy1, Andrew E Parker, Luke A J O'Neill
1Trinity College Dublin,School of Biochemistry and Immunology, Dublin 2, Ireland.
Abstract:
There is a growing interest in the targeting of Toll-like receptors (TLRs) for the prevention and treatment of cancer, rheumatoid arthritis, inflammatory bowel disease and systemic lupus erythematosus (SLE). Several new compounds are now undergoing preclinical and clinical evaluation, with a particular focus on TLR7 and TLR9 activators as adjuvants in infection and cancer, and inhibitors of TLR2, TLR4, TLR7 and TLR9 for the treatment of sepsis and inflammatory diseases. Here, we focus on TLRs that hold the most promise for drug discovery research, highlighting agents that are in the discovery phase and in clinical trials,and on the emerging new aspects of TLR-mediated signalling - such as control by ubiquitination and regulation by microRNAs - that might offer further possibilities of therapeutic manipulation.
Insights
Targeting Toll-like receptors (TLRs) shows promise for treating cancer and inflammatory diseases. Research focuses on TLR7 and TLR9 activators and inhibitors, with new signaling insights offering therapeutic potential.
Area of Science:
- Immunology
- Pharmacology
- Drug Discovery
Background:
- Growing interest in targeting Toll-like receptors (TLRs) for various diseases.
- TLRs play crucial roles in immune responses and disease pathogenesis.
- Existing research focuses on specific TLRs for therapeutic interventions.
Purpose of the Study:
- To review TLRs with the most promise for drug discovery.
- To highlight agents in discovery and clinical trials.
- To explore emerging aspects of TLR-mediated signaling for therapeutic manipulation.
Main Methods:
- Literature review of preclinical and clinical studies.
- Focus on TLR7 and TLR9 activators and inhibitors.
- Examination of novel signaling pathways like ubiquitination and microRNAs.
Main Results:
- Several compounds targeting TLRs are in preclinical and clinical evaluation.
- TLR7 and TLR9 activators are explored as adjuvants for infection and cancer.
- TLR2, TLR4, TLR7, and TLR9 inhibitors are investigated for sepsis and inflammatory diseases.
Conclusions:
- Targeting TLRs offers significant therapeutic potential for cancer and inflammatory conditions.
- Emerging insights into TLR signaling, including ubiquitination and microRNAs, present new avenues for drug development.
- Continued research into TLR modulation is crucial for advancing treatment strategies.
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