ArticleThe Journal of cell biology2009
Glyburide inhibits the Cryopyrin/Nalp3 inflammasome.
Article in The Journal of cell biology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 472 papers, 2 of them syntheses that pooled it.
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Who cites it
472 citing papers in PubMed, 2 syntheses or guidelines pooled it, 802 citations in OpenAlex.
- The Role of NLRP3 Inflammasome in Obesity and PCOS-A Systematic Review and Meta-Analysis.International journal of molecular sciences · 2023Pooled it
- Inflammasome Targeted Therapy as Novel Treatment Option for Aortic Aneurysms and Dissections: A Systematic Review of the Preclinical Evidence.Frontiers in cardiovascular medicine · 2021Pooled it
- Inflammation as a therapeutic target to improve kidney and cardiovascular outcomes.Nature reviews. Nephrology · 2026Review
- Sulfonylurea receptor 1 deficiency alleviates acute lung injury by activating PARP1 in epithelial cells.iScience · 2026Article
- Role of NLRP3 Inflammasome Inhibitors in Endothelial Dysfunction and Vascular Repair.Antioxidants (Basel, Switzerland) · 2026Review
- Mechanisms and reversal strategies of liver fibrosis: from regulation of cell fate to clinical translation.Journal of translational medicine · 2026Review
- Review on the Mechanism of and Therapies Targeting PANoptosis in Ulcerative Colitis.Biomolecules · 2026Review
- Regulated necrosis at the crossroads of liver inflammation and cancer development.Nature reviews. Gastroenterology & hepatology · 2026Review
- The NLRP3 Inflammasome: Mechanisms of Activation, Regulation, and Therapeutic Opportunities.MedComm · 2026Review
- Cell death in multiple sclerosis.Cell death and differentiation · 2026Review
- [Immunometabolic disorders in type 2 diabetes mellitus mediated by NLRP3 inflammasome activation and methods of pharmacological correction thereof].Problemy endokrinologii · 2026Review
- NLRP3 Inflammasome and Polycystic Ovary Syndrome (PCOS): A Novel Profile in Adipose Tissue.International journal of molecular sciences · 2026Article
- Immune dysregulation in chronic diabetic wounds: therapeutic opportunities for healing reprogramming.Frontiers in immunology · 2026Review
- Targeting inflammasome, IL-1β, and coagulation in melioidosis.Frontiers in microbiology · 2026Review
- NLRP3 inflammasome in acute kidney injury: molecular mechanisms, post-translational regulation, and immunotherapeutic potential.Frontiers in immunology · 2026Review
- Clinical efficacy of guided tissue regeneration combined with orthodontic treatment on periodontitis.Frontiers in bioengineering and biotechnology · 2026Article
- Pyroptosis-induced tissue damage in kidney disease.Renal failure · 2025Review
- Targeting PANoptosis: a promising therapeutic strategy for ALI/ARDS.Apoptosis : an international journal on programmed cell death · 2025Review
- Carbutamide, an Obsolete Anti-Diabetic Drug, Has Potential as a Potent Anticolitic Agent via Azo-Conjugation with Mesalazine.Pharmaceutics · 2025Article
- Discovery of potent and selective inhibitors of human NLRP3 with a novel mechanism of action.The Journal of experimental medicine · 2025Article
412 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
Inflammasomes activate caspase-1 for processing and secretion of the cytokines interleukin-1beta (IL-1beta) and IL-18. Cryopyrin/NALP3/NLRP3 is an essential component of inflammasomes triggered by microbial ligands, danger-associated molecular patterns (DAMPs), and crystals. Inappropriate Cryopyrin activity has been incriminated in the pathogenesis of gouty arthritis, Alzheimer's, and silicosis. Therefore, inhibitors of the Nalp3 inflammasome offer considerable therapeutic promise. In this study, we show that the type 2 diabetes drug glyburide prevented activation of the Cryopyrin inflammasome. Glyburide's cyclohexylurea group, which binds to adenosine triphosphatase (ATP)-sensitive K(+) (K(ATP)) channels for insulin secretion, is dispensable for inflammasome inhibition. Macrophages lacking K(ATP) subunits or ATP-binding cassette transporters also activate the Cryopyrin inflammasome normally. Glyburide analogues inhibit ATP- but not hypothermia-induced IL-1beta secretion from human monocytes expressing familial cold-associated autoinflammatory syndrome-associated Cryopyrin mutations, thus suggesting that inhibition occurs upstream of Cryopyrin. Concurrent with the role of Cryopyrin in endotoxemia, glyburide significantly delays lipopolysaccharide-induced lethality in mice. Therefore, glyburide is the first identified compound to prevent Cryopyrin activation and microbial ligand-, DAMP-, and crystal-induced IL-1beta secretion.
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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.