ArticleEMBO reports2023
Mefloquine targets NLRP3 to reduce lipopolysaccharide-induced systemic inflammation and neural injury.
Article in EMBO reports, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 9 citations in OpenAlex.
- AMPK-NLRP3 Inflammasome Crosstalk: Structural Insights, Molecular Mechanisms, and Therapeutic Implications for Inflammation and Neuroinflammation.Molecular neurobiology · 2026Review
- Macrophage piezo1 senses mechanical force to drive osteoclastogenesis via ZBP1: Implications for bone remodelling therapy.Clinical and translational medicine · 2026Article
- High-Throughput Screening Reveals That CeeNU Acts as a New NLRP3 Inflammasome Inhibitor.MedComm · 2026Article
- FDA-approved drug library screen identifies antidepressants, antimicrobials, anti-COPD, and anti-CVD agents as blockers of NLRP3 inflammasome and sepsis in a sex-dependent manner.bioRxiv : the preprint server for biology · 2026Article
- Extracellular LCN2 Binding to 24p3R in Astrocytes Impedes α-Synuclein Endocytosis in Parkinson's Disease.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- The Protective Role of Baicalin in the Regulation of NLRP3 Inflammasome in Different Diseases.Cell biochemistry and biophysics · 2025Review
- Astrocyte-derived CCL5-mediated CCR5Science advances · 2025Article
- Inactivation of NLRP3 inflammasome by dephosphorylation at Serine 658 alleviates glial inflammation in the mouse model of Parkinson's disease.Molecular neurodegeneration · 2025Article
- Progress in the study of mefloquine as an antibiotic adjuvant for combination bacterial inhibition treatment.Frontiers in cellular and infection microbiology · 2024Review
- Mefloquine targets NLRP3 to reduce lipopolysaccharide-induced systemic inflammation and neural injury.EMBO reports · 2023Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
The NLR family pyrin domain containing 3 (NLRP3) inflammasome plays an important role in the pathogenesis of a wide variety of human diseases. So far, drugs directly and specifically targeting the NLRP3 inflammasome are not available for clinical use since the safety and efficacy of new compounds are often unclear. A promising approach is thus to identify NLRP3 inhibitors from existing drugs that are already in clinical use. Here, we show that mefloquine, a well-known antimalarial drug, is a highly selective and potent NLRP3 inhibitor by screening a FDA-approved drug library. Mechanistically, mefloquine directly binds to the NLRP3 NACHT and LRR domains to prevent NLRP3 inflammasome activation. More importantly, mefloquine treatment attenuates the symptoms of lipopolysaccharide-induced systemic inflammation and Parkinson's disease-like neural damage in mice. Our findings identify mefloquine as a potential therapeutic agent for NLRP3-driven diseases and migth expand its clinical use considerably.
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