NLRP3 inhib 
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  • ||||||||||  Retrospective data, Review, Journal:  The Effects of NLRP3 Inflammasome Inhibition in Experimental Acute Pancreatitis: A Systematic Review and Meta-Analysis. (Pubmed Central) -  Mar 23, 2022   
    In addition, inhibition of NLRP3 inflammasome reduced the levels of circulating inflammatory cytokines, as well as mitigating severity of AP-associated acute lung injury and acute intestinal injury. To conclude, inhibition of NLRP3 inflammasome has protective effects on AP by mitigating organ injury and systemic inflammation in animal studies, indicating that NLRP3 inflammasome holds promise as a target for specific AP therapy.
  • ||||||||||  TIMP2 ATTENUATES INFLAMMATORY RESPONSE IN SEPSIS-INDUCED ACUTE KIDNEY INJURY ([VIRTUAL]) -  Mar 23, 2022 - Abstract #SCCM2022SCCM_2361;    
    Kidney injury scores of TIMP2 −/− mice were also significantly higher than that of WT mice (p< 0.05). Furthermore, the serum levels of IL-1β of TIMP2 −/− mice were higher than that of WT post CLP and LPS treatment.
  • ||||||||||  Journal:  Euphzycopias A-I, macrocyclic diterpenes with NLRP3 inflammasome inhibitory activity from Euphorbia helioscopia L. (Pubmed Central) -  Mar 18, 2022   
    A phytochemical investigation was conducted on Euphorbia helioscopia, resulting in the isolation of thirteen compounds, including nine undescribed diterpenoids, Euphzycopias A - I (1-9), of which the skeletons of compounds 1-4 were found in E. helioscopia L. Compounds 1-3 had 5/7/6 cyclic systems, while compound 4 had a 4/11 polycyclic system with a 4,7-cyclic ether between C-4 and C-7. The anti-inflammasome test using the isolated compounds (1-6, 8-13) showed that the diterpenes from E. helioscopia L. had a strong inhibitory effect on NLRP3 inflammasomes with IC values of 3.34-14.92 μM.
  • ||||||||||  colchicine / Generic mfg.
    Clinical, Review, Journal:  Colchicine for COVID-19: targeting NLRP3 inflammasome to blunt hyperinflammation. (Pubmed Central) -  Mar 18, 2022   
    This may occur through a selective blockade of different steps preceding NLRP3 inflammasome oligomerization as well as through a reduced release of the main cytokines (IL-1β and IL-18). Since most evidence is based on observational studies, definitive conclusion cannot be drawn and additional studies are needed to confirm preliminary results and further dissect how colchicine and other NLRP3 inhibitors reduce the inflammatory burden and evaluate the timing and duration of treatment.
  • ||||||||||  Review, Journal:  The potential of probiotics in the amelioration of hyperuricemia. (Pubmed Central) -  Mar 18, 2022   
    We propose that future research should focus on superior strain resource isolation and insight into the cause-effect mechanisms of probiotics for hyperuricemia amelioration. The safety and effects of the application of probiotics in clinical use also need verification.
  • ||||||||||  TriptoSar (triptolide) / Pierre Fabre
    Review, Journal:  Phenols and terpenoids: natural products as inhibitors of NLRP3 inflammasome in cardiovascular diseases. (Pubmed Central) -  Mar 16, 2022   
    Thus, 20 natural products from phenols and terpenoids for the treatment of cardiovascular disease based on the inhibition of NLRP3 inflammasome were summarized and screened. Docking results showed salvianolic acid B and ellagic acid in phenols, and oridonin and triptolide in terpenoids had a better binding activity with NLRP3, which can provide theoretical support for finding novel NLRP3 inflammasome inhibitors or lead compounds in the future.
  • ||||||||||  Journal:  Activation of NLRP3-Caspase-1 pathway contributes to age-related impairments in cognitive function and synaptic plasticity. (Pubmed Central) -  Mar 15, 2022   
    Furthermore, NLRP3 inflammasome inhibitor elevated the surface expression of AMPA receptor and the phosphorylated levels of CaMKII, CREB in hippocampus, and finally contributed to the attenuation of hippocampal long-term potentiation (LTP) deficits and the improvement of cognitive decline of natural aging rats. These results revealed an important role for the NLRP3-Caspase-1 pathway in aging-induced cognitive decline and suggested that inhibition of NLRP3 inflammasome represented a novel therapeutic intervention for aging-related cognitive impairment.
  • ||||||||||  Journal:  Licochalcone B specifically inhibits the NLRP3 inflammasome by disrupting NEK7-NLRP3 interaction. (Pubmed Central) -  Mar 15, 2022   
    Furthermore, LicoB exhibits protective effects in mouse models of NLRP3 inflammasome-mediated diseases, including lipopolysaccharide (LPS)-induced septic shock, MSU-induced peritonitis and non-alcoholic steatohepatitis (NASH). Our findings indicate that LicoB is a specific NLRP3 inhibitor and a promising candidate for treating NLRP3 inflammasome-related diseases.
  • ||||||||||  Bay11-7082 / InvivoGen, Mifeprex (mifepristone) / Danco Laboratories
    Journal:  NLRP3 inflammasome is involved in uterine activation for labor at term and preterm. (Pubmed Central) -  Mar 12, 2022   
    MCC950 postponed labor onset of the mice with LPS and RU38486 treatment and inhibited NLRP3 inflammasome activation in uterus. Our data provide the evidence that NLRP3 inflammasome is involved in uterine activation for labor onset in term and PTB in humans and mouse model.
  • ||||||||||  NLPR3-INFLAMMASOME INHIBITION AMELIORATES SECONDARY INFARCT GROWTH IN SUBACUTE ISCHEMIC STROKE IN MICE (E-POSTER LIBRARY) -  Mar 12, 2022 - Abstract #ESOC2022ESOC_1004;    
    In line with our previous results showing a significant impact of the NLRP3-inhibition on post-stroke outcome after an observation period of 1d, our results underline the role of the NLRP3-inflammasome as master-switch of inflammation during IS. Of note, not only the hyperacute but also the delayed treatment after reperfusion lead to better post-stroke outcomes and smaller infarct sizes that persisted for a whole week.
  • ||||||||||  Journal:  Identification of NLRP3 Homo-Oligomerization Inhibitors with Anti-Inflammatory Activity. (Pubmed Central) -  Mar 12, 2022   
    Our results demonstrate that these NLRP3 inhibitors interfere with ASC speck formation, inhibit pro-inflammatory cytokine IL1-β release, and decrease pyroptotic cell death. We employed spectroscopic techniques and computational docking analyses with QM380 and QM381 and the PYD domain to confirm the experimental results and predict possible mechanisms underlying the inhibition of NLRP3 homo-interactions.
  • ||||||||||  NOVEL NLRP3 INHIBITORS AS POTENTIAL THERAPEUTICS FOR ALZHEIMER'S DISEASE (HALL C) -  Mar 9, 2022 - Abstract #ADPD2022ADPD_1029;    
    In conclusion, a novel scaffold was identified with unique binding interactions to the LRR domain of NLRP3, and the flexibility to provde both covalent and noncovalent NLRP3 inhibitors. Medicinal chemistry studies confirmed that the scaffold can be optimized to improve inhibitory potency and binding affinity to the NLRP3 protein, and new lead NLRP3 inhibitors have been identified for further development.
  • ||||||||||  Deciphering role of NLRP3 inflammasome in acute myeloid leukemia microenvironment (E-Poster Website) -  Mar 9, 2022 - Abstract #AACR2022AACR_7130;    
    Paraffin sections of AML BM are being evaluated for NLRP3 pathway markers by immunohistochemistry. Understanding remodelling of BM-MSC, leukemia target and immune cell dynamics through NLRP3 pathway regulation in stroma microenvironment may provide crucial leads in therapeutic modulation of the immune response within the stem cell niche.
  • ||||||||||  Journal:  SARS-CoV-2 viroporin encoded by ORF3a triggers the NLRP3 inflammatory pathway. (Pubmed Central) -  Mar 8, 2022   
    Importantly, infection of epithelial cells with SARS-CoV-2 similarly activates the NLRP3 inflammasome. With the NLRP3 inhibitor MCC950 and select FDA-approved oral drugs able to block ORF3a-mediated inflammasome activation, as well as key ORF3a amino acid residues needed for virus release and inflammasome activation conserved in the new variants of SARS-CoV-2 isolates across continents, ORF3a and NLRP3 present prime targets for intervention.
  • ||||||||||  RRx-001 / EpicentRx
    Journal:  An RRx-001 Analogue With Potent Anti-NLRP3 Inflammasome Activity but Without High-Energy Nitro Functional Groups. (Pubmed Central) -  Mar 8, 2022   
    Furthermore, treatment with 149-01 effectively alleviate the severity of several inflammatory diseases in mice, including lipopolysaccharide (LPS)-induced systemic inflammation, monosodium urate crystals (MSU)-induced peritonitis and experimental autoimmune encephalomyelitis (EAE). Thus, our results indicate that 149-01 is a potential lead for developing therapeutic agent for NLRP3-related inflammatory diseases.
  • ||||||||||  Inflammasome inhibitors for the treatment of muscular dystrophies () -  Mar 6, 2022 - Abstract #AAN2022AAN_2287;    
    These data were replicated with success in C2C12 murine myoblasts and in human myotubes. This molecule could thus offer promising therapeutic prospects for managing DMD or other muscle and inflammatory disorders.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Calycosin Alleviates Doxorubicin-Induced Cardiotoxicity and Pyroptosis by Inhibiting NLRP3 Inflammasome Activation. (Pubmed Central) -  Mar 5, 2022   
    In vivo, CAL afforded a protective effect against DOX-induced cardiac injury by improving myocardial function, inhibiting brain natriuretic peptide, and improving the changes of the histological morphology of DOX-treated mice. Collectively, our findings confirmed that CAL alleviates DOX-induced cardiotoxicity and pyroptosis by inhibiting NLRP3 inflammasome activation in vivo and in vitro.