ArticleCellular & molecular immunology2021
RRx-001 ameliorates inflammatory diseases by acting as a potent covalent NLRP3 inhibitor.
Article in Cellular & molecular immunology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 77 papers.
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Who cites it
77 citing papers in PubMed, 125 citations in OpenAlex.
- Ciclopirox Olamine Inhibits the NLRP3 Inflammasome to Alleviate Inflammatory Diseases.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- High-Throughput Screening Reveals That CeeNU Acts as a New NLRP3 Inflammasome Inhibitor.MedComm · 2026Article
- ML364 ameliorates NLRP3-induced inflammatory response.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2026Article
- Progress in the Treatment of Ulcerative Colitis by Targeting NLRP3 Inflammasome.Drug design, development and therapy · 2026Review
- ML345 is a potent and selective NLRP3 inflammasome inhibitor with anti-inflammatory activity.Molecular biomedicine · 2025Article
- Pinosylvin Inhibits Inflammatory and Osteoclastogenesis via NLRP3 Inflammasome.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- New Insights on the Potential Role of Pyroptosis in Parkinson's Neuropathology and Therapeutic Targeting of NLRP3 Inflammasome with Recent Advances in Nanoparticle-Based miRNA Therapeutics.Molecular neurobiology · 2025Review
- Immune cell metabolism in cancer drug resistance: Advances in target discovery and clinical translation.Chinese journal of cancer research = Chung-kuo yen cheng yen chiu · 2025Article
- Research Progress in the Molecular Mechanism of NLRP3 Inflammasome in Alzheimer's Disease and Regulation by Natural Plant Products.Molecular neurobiology · 2025Review
- Updated insights into the molecular networks for NLRP3 inflammasome activation.Cellular & molecular immunology · 2025Review
- Targeting the NLRP3 inflammasome for inflammatory disease therapy.Trends in pharmacological sciences · 2025Review
- Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly.Nature communications · 2025Article
- Targeting cholesterol-driven pyroptosis: a promising strategy for the prevention and treatment of atherosclerosis.Molecular biology reports · 2025Review
- NLRP3 Inflammasome in Vascular Dementia: Regulatory Mechanisms, Functions, and Therapeutic Implications: A Comprehensive Review.CNS neuroscience & therapeutics · 2025Review
- A small molecule directly targets NLRP3 to promote inflammasome activation and antitumor immunity.Cell death & disease · 2025Article
- A review on NLRP3 inflammasome modulation by animal venom proteins/peptides: mechanisms and therapeutic insights.Inflammopharmacology · 2025Review
- Lactylation in cancer: metabolic mechanism and therapeutic strategies.Cell death discovery · 2025Review
- Targeting NLRP3 Inflammasomes: A Trojan Horse Strategy for Intervention in Neurological Disorders.Molecular neurobiology · 2025Review
- Biological and therapeutic significance of targeting NLRP3 inflammasome in the brain and the current efforts to develop brain-penetrant inhibitors.Advances in pharmacology (San Diego, Calif.) · 2025Review
- Inflammasomes in Intestinal Disease: Mechanisms of Activation and Therapeutic Strategies.International journal of molecular sciences · 2024Review
17 more citing papers are in PubMed but not listed here.
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The NLRP3 inflammasome plays a crucial role in innate immune-mediated inflammation and contributes to the pathogenesis of multiple autoinflammatory, metabolic and neurodegenerative diseases, but medications targeting the NLRP3 inflammasome are not available for clinical use. RRx-001 is a well-tolerated anticancer agent currently being investigated in phase III clinical trials, but its effects on inflammatory diseases are not known. Here, we show that RRx-001 is a highly selective and potent NLRP3 inhibitor that has strong beneficial effects on NLRP3-driven inflammatory diseases. RRx-001 inhibits the activation of the canonical, noncanonical, and alternative NLRP3 inflammasomes but not the AIM2, NLRC4 or Pyrin inflammasomes. Mechanistically, RRx-001 covalently binds to cysteine 409 of NLRP3 via its bromoacetyl group and therefore blocks the NLRP3-NEK7 interaction, which is critical for the assembly and activation of the NLRP3 inflammasome. More importantly, RRx-001 treatment attenuates the symptoms of lipopolysaccharide (LPS)-induced systemic inflammation, dextran sulfate sodium (DSS)-induced colitis and experimental autoimmune encephalomyelitis (EAE) in mice. Thus, our study identifies RRx-001 as a new potential therapeutic agent for NLRP3-driven 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.