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  • ||||||||||  Journal:  An Overview of Disease Models for NLRP3 Inflammasome Over-activation. (Pubmed Central) -  Oct 16, 2021   
    The potential risk for cross-reaction is high; therefore, the development of highly specific inhibitors is essential. The selection of appropriate cell and animal models, and combined use of different models for the evaluation of these inhibitors can help to clarify the target specificity and therapeutic effects, which is beneficial for the development and application of drugs targeting the NLRP3 inflammasome.
  • ||||||||||  Journal:  NLRP3 Inflammasome Promotes the Progression of Acute Myeloid Leukemia via IL-1β Pathway. (Pubmed Central) -  Oct 16, 2021   
    In AML murine model, up-regulation of NLRP3 increases the leukemia burden in bone marrow, spleen and liver, and shortens the survival time; furthermore, knocking out NLRP3 inhibits leukemia progression. Collectively, all these evidences demonstrate that NLRP3 inflammasome promotes AML progression in an IL-1β dependent manner, and targeting NLRP3 inflammasome may provide a novel therapeutic option for AML.
  • ||||||||||  Preclinical, Journal:  Atractylenolide III reduces NLRP3 inflammasome activation and Th1/Th2 imbalances in both in vitro and in vivo models of asthma. (Pubmed Central) -  Oct 14, 2021   
    In ovalbumin-induced asthmatic mice, atractylenolide III treatment also significantly inhibited NLRP3 inflammasome activation and restored the Th1/Th2 balance. These results indicate that atractylenolide III reduced NLRP3 inflammasome activation and regulated the Th1/Th2 balance in IL-4 induced 16HBE cells and ovalbumin-induced asthmatic mice, suggesting it has a protective effect that may be useful in the treatment of pediatric asthma.
  • ||||||||||  Journal:  Necrosulfonamide reverses pyroptosis-induced inhibition of proliferation and differentiation of osteoblasts through the NLRP3/caspase-1/GSDMD pathway. (Pubmed Central) -  Oct 13, 2021   
    The fact that overexpression of caspase-1, gasdermin D (GSDMD) and NLRP3 abolished the effects of NSA on the viability and pyroptosis of osteoblasts, as well as the mRNA expression of differentiation-related genes and the activity of ALP in osteoblasts, indicated that NSA promoted the proliferation and differentiation of osteoblasts by inhibiting the NLRP3/caspase-1/GSDMD pyroptosis pathway. The present study provides proof supporting the potential application of NSA for improving the function of osteoblasts in fracture repair and indicates the value of the NLRP3/caspase-1/GSDMD pyroptosis pathway as a pharmaceutical target.
  • ||||||||||  glibenclamide / Generic mfg.
    Preclinical, Journal:  An in vitro study of ApxI from Actinobacillus pleuropneumoniae serotype 10 and induction of NLRP3 inflammasome-dependent cell death. (Pubmed Central) -  Oct 12, 2021   
    Glyburide and MCC950 were used to inhibit the NLRP3 inflammasome...Detection of caspase-1 in alveolar macrophages was higher after ApxI treatment and it was blocked by MCC950 or heat inactivation. To the best of the authors' knowledge, we have described for the first time in vitro induction of ApxI associated pyroptosis in alveolar macrophages and endothelial cells, a rapid cell death that depends on the activation of caspase-1 via the NLRP3 inflammasome.
  • ||||||||||  Review, Journal:  Targeting NLRP3 Inflammasome in the Treatment Of Diabetes and Diabetic Complications: Role of Natural Compounds from Herbal Medicine. (Pubmed Central) -  Oct 12, 2021   
    In this review, we summarized the role of NLRP3 inflammasome in diabetes and several diabetic complications, as well as 31 active compounds that exert therapeutic effect on diabetic complications via inhibiting NLRP3 inflammasome. Improving our understanding of these promising candidates from natural compounds in herbal medicine targeting NLRP3 inflammasome inspires us the relationship between inflammation and metabolic disorders, and also sheds light on searching potential agents or therapies in the treatment of diabetes and diabetic complications.
  • ||||||||||  Journal:  miR-30c-5p Alleviated Pyroptosis During Sepsis-Induced Acute Kidney Injury via Targeting TXNIP. (Pubmed Central) -  Oct 9, 2021   
    Upregulation of miR-30c-5p repressed the expression of TXNIP, which inhibited NLRP3, ASC, and caspase-1 expression, as well as secretion of inflammatory cytokines. In conclusion, our data suggested that miR-30c-5p negatively controlled the NLRP3 signal pathway-related pyroptosis and sepsis-induced injury via TXNIP, indicating that this axis might be a positive therapeutic target for the patient with SAKI.
  • ||||||||||  Preclinical, Journal:  Sinomenine Alleviates Murine Experimental Autoimmune Encephalomyelitis Model of Multiple Sclerosis through Inhibiting NLRP3 Inflammasome. (Pubmed Central) -  Oct 7, 2021   
    Furthermore, immunoreactivity for MBP decreased and increased for GFAP and Iba1 after MOG-immunization, which was in part reversed upon sinomenine administration. Overall, sinomenine decreases EAE severity, which is attributed to its alleviation of microglial and astrocytic mobilization, demyelination, and axonal damage along with its suppression of neuroinflammation, and its beneficial effect is also associated with its inhibitory effects on inflammasome and pyroptotic pathways; this may be of potential benefit for the primary progressive phenotype of MS.
  • ||||||||||  Ocaliva (obeticholic acid) / Intercept
    Journal:  A new mechanism of obeticholic acid on NASH treatment by inhibiting NLRP3 inflammasome activation in macrophage. (Pubmed Central) -  Oct 7, 2021   
    Overall, sinomenine decreases EAE severity, which is attributed to its alleviation of microglial and astrocytic mobilization, demyelination, and axonal damage along with its suppression of neuroinflammation, and its beneficial effect is also associated with its inhibitory effects on inflammasome and pyroptotic pathways; this may be of potential benefit for the primary progressive phenotype of MS. This finding brings up a new mechanism of OCA on NASH treatment, suggested by direct inhibition on NLRP3 inflammasome activation in macrophage, further suppression on inflammasome activation-elicited hepatic lipid accumulation, and contributing to the amelioration of NASH.
  • ||||||||||  vincristine / Generic mfg.
    Journal:  Vincristine-induced peripheral neuropathy is driven by canonical NLRP3 activation and IL-1β release. (Pubmed Central) -  Oct 6, 2021   
    Moreover, treatment with the IL-1 receptor antagonist anakinra prevented the development of vincristine-induced neuropathy without adversely affecting chemotherapy efficacy or tumor progression in patient-derived medulloblastoma xenograph models. These results detail the neuro-inflammatory mechanisms leading to vincristine-induced peripheral neuropathy and suggest that repurposing anakinra may be an effective co-treatment strategy to prevent vincristine-induced peripheral neuropathy.
  • ||||||||||  belnacasan (VX-765) / Vertex, setanaxib (GKT831) / Calliditas
    Journal:  NLR family pyrin domain containing 3 (NLRP3) and caspase 1 (CASP1) modulation by intracellular Cl concentration. (Pubmed Central) -  Oct 6, 2021   
    DCF fluorescence (cellular reactive oxygen species, cROS) and MitoSOX fluorescence (mitochondrial ROS, mtROS) also showed maximal ROS levels at 75 mM Cl , a response strongly inhibited by the ROS scavenger N-acetyl-L-cysteine (NAC) or the NADPH oxidase (NOX) inhibitor GKT137831...More importantly, the serum/glucocorticoid regulated kinase 1 (SGK1) inhibitor GSK650394, or its shRNAs, completely abrogated the IL-1β mRNA response to Cl and the IL-1β secretion, interrupting the autocrine IL-1β loop. The results suggest that Cl effects are mediated by SGK1, which under Cl modulation stimulates the secretion of mature IL-1β, in turn, responsible for the upregulation of ROS, CASP1, NLRP3, and IL-1β itself, through autocrine signaling.
  • ||||||||||  Kineret (anakinra) / SOBI, Arcalyst (rilonacept) / Regeneron, Kiniksa
    Review, Journal:  Interleukin-1 and the NLRP3 Inflammasome in Pericardial Disease. (Pubmed Central) -  Oct 3, 2021   
    NLRP3 inflammasome, a macromolecular structure sensing damage and releasing pro-inflammatory cytokines, is centrally involved as it releases interleukin (IL)-1β, whose auto-induction feeds an autoinflammatory disease, mostly responsible for recurrences. Colchicine, an inhibitor of NLRP3 inflammasome formation, and IL-1-targeted therapies, such as anakinra and rilonacept, were found to effectively blunt the acute inflammation and reduce the risk for recurrences.
  • ||||||||||  Review, Journal:  The NLRP3 inflammasome and COVID-19: Activation, pathogenesis and therapeutic strategies. (Pubmed Central) -  Oct 2, 2021   
    Furthermore, we describe the involvement of the NLRP3 inflammasome in the pathogenesis of COVID-19 (e.g., cytokine storm, respiratory manifestations, cardiovascular comorbidity and neurological symptoms). Finally, we also propose several promising inhibitors targeting the NLRP3 inflammasome, cytokine products and neutrophils to provide novel therapeutic strategies for COVID-19.
  • ||||||||||  Review, Journal:  Medicinal plants and bioactive natural products as inhibitors of NLRP3 inflammasome. (Pubmed Central) -  Oct 1, 2021   
    Therefore, this review focuses on the effects of nutraceuticals and bioactive compounds derived from medicinal plants on NLRP3 inflammasome activation and the possible mechanisms of action of these natural products. Thus, herb-based, natural products/compounds can be considered novel, practical, and accessible agents in chronic inflammatory diseases by inhibiting NLRP3 inflammasome activation.
  • ||||||||||  Preclinical, Journal:  Microglial autophagy defect causes parkinson disease-like symptoms by accelerating inflammasome activation in mice. (Pubmed Central) -  Sep 30, 2021   
    Interestingly, we found that serum MIF levels in PD patients were significantly elevated. Taken together, our results reveal an important role of autophagy in microglial activation-driven PD-like symptoms, thus providing potential targets for the clinical treatment of PD.Abbreviations: ATG: autophagy related; cAMP: cyclic adenosine monophosphate; cKO: conditional knockout; NOS2/INOS: nitric oxide synthase 2, inducible; IL1B: interleukin 1 beta; ITGAM/CD-11b: integrin alpha M/cluster of differentiation molecule 11B; MAP1LC3: microtubule-associated protein 1 light chain 3; MIF: macrophage migration inhibitory factor (glycosylation-inhibiting factor); NLRP3: NLR family pyrin domain containing 3; PBS: phosphate-buffered saline; PD: parkinson disease; PDE10A: phosphodiesterase 10A; SN: substantial nigra; TH: tyrosine hydroxylase; TNF: tumor necrosis factor; WT: wild type.
  • ||||||||||  rosiglitazone / Generic mfg.
    Preclinical, Journal:  Rosiglitazone ameliorates radiation-induced intestinal inflammation in rats by inhibiting NLRP3 inflammasome and TNF-α production. (Pubmed Central) -  Sep 29, 2021   
    MSU reversed the protective effect of rosiglitazone on radiation-induced intestinal injury in rats by reversing the rosiglitazone-induced inhibition of IL-1β and TNF-α. Taken together, these findings indicate that the peroxisome proliferator-activated receptor gamma (PPARγ) agonist, rosiglitazone, ameliorates radiation-induced intestine inflammation in rats via inhibiting the induction of the NLRP3-dependent inflammasome in macrophages.
  • ||||||||||  minocycline / Generic mfg.
    Preclinical, Journal:  The critical role of the hippocampal NLRP3 inflammasome in social isolation-induced cognitive impairment in male mice. (Pubmed Central) -  Sep 29, 2021   
    Minocycline is an antibiotic that limits microglia responses, and previous study also showed that minocycline could prevent stress-induced pro-inflammatory cytokine expression in the brain...Furthermore, alterations in SI mice were also restored by chronic treatment with the NLRP3 inhibitor MCC950. These results indicate that the microglia-derived NLRP3 inflammasome may be primarily involved in the inflammatory response to social isolation and that specific NLRP3 inflammasome inhibition using MCC950 may represent a promising therapeutic approach for early stress induced cognitive impairment.
  • ||||||||||  azacitidine / Generic mfg.
    [VIRTUAL] THE QUEST FOR DISEASE MODIFICATION IN LOWER RISK MDS VIA TARGETING OF INFLAMMATORY SIGNALING () -  Sep 26, 2021 - Abstract #MDS2021MDS_288;    
    Additionally, activating both innate and adaptive immune responses, as is being evaluated with therapies targeting CD47 and TIM-3, has shown synergistic activity in combination with azacitidine in higher risk MDS patients but may also play a critical role to improve long term outcomes in lower risk MDS patients. Ultimately, combination trials may be required to change the natural history of MDS patients with significant optimism on the future treatment landscape.
  • ||||||||||  Review, Journal:  The NLRP3 inflammasome: Mechanism of action, role in disease and therapies. (Pubmed Central) -  Sep 26, 2021   
    Growing evidence has indicated hyperactivation of NLRP3 inflammasome is involved in a wide range of inflammatory diseases. In this review we present the recent advances in understanding the mechanism of NLRP3 activation, its role in driving inflammatory diseases, and the development of NLRP3 targeted therapies.
  • ||||||||||  Journal:  Specific NLRP3 Inhibition Protects Against Diabetes-Associated Atherosclerosis. (Pubmed Central) -  Sep 26, 2021   
    In a range of cell lines (murine bone marrow-derived macrophages (BMDMs), human monocytic THP-1 cells, PMA-differentiated human macrophages and diabetic human aortic smooth muscle cells (AoSMCs)), MCC950 significantly reduced IL-1β and/or caspase-1 secretion and attenuated leukocyte-SMC interactions under high glucose or LPS conditions. In summary, MCC950 reduces plaque development, promotes plaque stability and improves vascular function, suggesting that targeting NLRP3-mediated inflammation is a novel therapeutic strategy to improve diabetes-associated vascular disease.
  • ||||||||||  colchicine / Generic mfg.
    Journal:  Progress in the relationship between NLRP3 inflammasome and lung injury in COVID-19 (Pubmed Central) -  Sep 25, 2021   
    MCC950, colchicine and other NLRP3 inflammasome inhibitors, have been widely used in the treatment of various inflammatory diseases, and are currently in clinical trials for the treatment of COVID-19 patients. Here we reviewed the pathogenesis of COVID-19 and the SARS-CoV activation pathway of NLRP3 inflammasome, in order to reveal the role and mechanism of NLRP3 inflammasome in the process of SARS-CoV-2 infection, and provide a theoretical basis for the development of related targeted drugs.
  • ||||||||||  belnacasan (VX-765) / Vertex
    [VIRTUAL] Reperfusion Injury is Reduced by Antagonism of NLRP3's Caspase-1 (ePosters) -  Sep 24, 2021 - Abstract #AHA2021AHA_3968;    
    These results strongly support NLRP3 as the source of the lethal cas-1. VX-765 at reperfusion is a promising adjunct intervention to decrease infarct size in patients treated for ST-segment elevation myocardial infarction.