NLRP3 inhib 
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  • ||||||||||  TriptoSar (triptolide) / Pierre Fabre
    Journal:  The role of inflammasome activation in Triptolide-induced acute liver toxicity. (Pubmed Central) -  Feb 15, 2020   
    Taken together, our results revealed that activation of inflammasome aggravated the acute liver toxicity induced by TP. Inhibition of inflammasome could serve as a novel therapeutic target for the amelioration of TP-induced hepatotoxicity.
  • ||||||||||  Journal:  NLRP3 inflammasome mediate palmitate-induced endothelial dysfunction. (Pubmed Central) -  Feb 15, 2020   
    Inhibition of NLRP3 reduces SIRS and CARS, and might be used to treat patients with severe pancreatitis. NLRP3 inflammasome activation via AMPKα inactivation mediated palmitate-induced endothelial dysfunction through involves IL-1β-induced insulin signal pathway.
  • ||||||||||  Review, Journal:  The rOX-stars of inflammation: links between the inflammasome and mitochondrial meltdown. (Pubmed Central) -  Feb 15, 2020   
    Here, we review the features of mitochondria that drive inflammatory signalling, with a particular focus on mitochondrial activation of the NLRP3 inflammasome. Given that mitochondrial network dynamics, metabolic activity and redox state are all intricately linked to each other and to NLRP3 inflammasome activity, we highlight the importance of a holistic approach to investigations of NLRP3 activation by dysfunctional mitochondria.
  • ||||||||||  allopurinol / Generic mfg.
    Preclinical, Journal:  Curcumin attenuates potassium oxonate-induced hyperuricemia and kidney inflammation in mice. (Pubmed Central) -  Feb 14, 2020   
    Administration with CUR (20 or 40 mg/kg) or allopurinol (ALL, 5 mg/kg) was given to mice orally one hour later after the injection of potassium oxonate (PO) (300 mg/kg, i.p.) for 14 days...Further studies showed that CUR decreased inflammatory cytokines productions (IL-1β, IL-18) in serum, as well as inhibited PO-induced the activation of NLRP3 inflammasome signaling in the kidney. In conclusion, the study revealed that CUR exhibited anti-hyperuricemic and anti-inflammatory effects through suppressing NLRP3 inflammasome activation in kidney and provided the evidence for treating hyperuricemia and associated renal inflammation.
  • ||||||||||  Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Byetta (exenatide) / AstraZeneca
    Journal:  DPP-4 inhibition by linagliptin prevents cardiac dysfunction and inflammation by targeting the Nlrp3/ASC inflammasome. (Pubmed Central) -  Feb 14, 2020   
    Lina and EX had similar effects on IS and post-infarction function, but Lina attenuated the activation of the inflammasome and the upregulation of collagen-1 and collagen-3 more than direct GLP-1 receptor activation. This effect depends on p38 activation with downstream upregulation of miR-146b levels that suppresses TLR4 expression.
  • ||||||||||  Journal:  The reduction of XIAP is associated with inflammasome activation in RPE: implications for AMD pathogenesis. (Pubmed Central) -  Feb 14, 2020   
    This effect depends on p38 activation with downstream upregulation of miR-146b levels that suppresses TLR4 expression. Together, these data suggest XIAP-mediated inhibition of inflammasome activity in RPE may provide insights into the biological consequences of inflammasome activation in RPE and reveals the caspase-1/XIAP/IL-1β/IL-18 axis as a target for broader applications in AMD biology and treatment design.
  • ||||||||||  Journal:  Association of NLRP3 and CARD8 inflammasome polymorphisms with aseptic loosening after primary total hip arthroplasty. (Pubmed Central) -  Feb 14, 2020   
    After adjustment for gender, age and follow-up, patients with combined wild type of both NLRP3 and CARD8 had significantly smaller odds for early implant loosening (odds ratio 0.33, p = 0.02). Investigated polymorphisms may influence several inflammatory pathways and contribute to the loosening of artificial implants with potential clinical significance for proper selection of patients and endoprostheses when planning elective total hip arthroplasty.
  • ||||||||||  Kolchin (colchicine) / Incepta
    Journal:  Cichorium intybus L. Extract Suppresses Experimental Gout by Inhibiting the NF-κB and NLRP3 Signaling Pathways. (Pubmed Central) -  Feb 14, 2020   
    In conclusion, our study suggested that high level of let-7f-5p alleviated inflammation in SLE-BMSCs at least partly through targeting NLRP3, highlighting let-7f-5p as a novel promising therapeutic strategy for SLE treatment. This study suggests that chicory extract and chicoric acid may be used as promising therapeutic agents against gout by inhibiting the NF-κB and NLRP3 signaling pathways.
  • ||||||||||  Radicava (edaravone) / Mitsubishi Tanabe, edaravone (MT-1186) / Mitsubishi Tanabe
    Preclinical, Journal:  Edaravone Administration Confers Neuroprotection after Experimental Intracerebral Hemorrhage in Rats via NLRP3 Suppression. (Pubmed Central) -  Feb 14, 2020   
    This study suggests that chicory extract and chicoric acid may be used as promising therapeutic agents against gout by inhibiting the NF-κB and NLRP3 signaling pathways. The present study demonstrated that edaravone conducted neuroprotection after ICH partially via suppressing NF-κB-dependent NLRP3 in microglia, which contributed a novel evidence for clinic usage of edaravone after ICH.
  • ||||||||||  Journal:  Biochanin A attenuates myocardial ischemia/reperfusion injury through the TLR4/NF-κB/NLRP3 signaling pathway. (Pubmed Central) -  Feb 14, 2020   
    The present study demonstrated that edaravone conducted neuroprotection after ICH partially via suppressing NF-κB-dependent NLRP3 in microglia, which contributed a novel evidence for clinic usage of edaravone after ICH. The present study is the first evidence demonstrating that BCA attenuated Ml/R injury through suppressing TLR4/NF-kB/NLRP3 signaling pathway-mediated anti-inflammation pathway.
  • ||||||||||  Review, Journal:  Effect and Regulation of the NLRP3 Inflammasome During Renal Fibrosis. (Pubmed Central) -  Feb 13, 2020   
    Based on this, the present review summarizes recent findings in regard to NLRP3 inflammasome functions during various kidney diseases, and these findings indicate that the NLRP3 inflammasome not only mediates the inflammatory response but is also associated with pyroptosis, mitochondrial regulation, and myofibroblast differentiation during renal fibrosis. These novel findings provide us with a more in-depth understanding of the pathogenesis of renal fibrosis and will aid in the identification of new targets that can be used for the prevention and treatment of this disease.
  • ||||||||||  Clinical, Journal, IO Biomarker:  Differential expression of genes associated with T lymphocytes function in septic patients with hypoxemia challenge. (Pubmed Central) -  Feb 13, 2020   
    Candidate genes were identified after adjustment for age, sex and presence of lymphopenia with significantly negative correlations with partial pressure of O in an arterial blood (PaO) and fraction of inspiration O (FiO) ratio, among which NLRP3, SOS1, ELF1 and STAT3 held an increasing expression in ex vivo validation while the others, PSMA5, CLEC4D, CD300A, PRKD2 and PSMA2 showed the opposite alteration from those in vivo. Higher illness severity and incidence of lymphopenia was observed following hypoxemia in sepsis and T cell-related gene signatures were associated with hypoxemia during sepsis.
  • ||||||||||  A Bioisosteric Approach to Novel NLRP3 Inflammasome Inhibitors (Exhibit Hall D, Pennsylvania Convention Center) -  Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_4015;    
    This bioisosteric investigation led to the discovery of a new class of small molecule NLRP3 inhibitors with improved potency and attractive lead-like characteristics. These are highly differentiated from other known NLRP3 inhibitors and offer scope for further optimisation.
  • ||||||||||  Novel ester-based NLRP3 inflammasome inhibitors (204B, Pennsylvania Convention Center) -  Feb 13, 2020 - Abstract #ACSSp2020ACS_Sp_1229;    
    The best compounds from this series are up to 20-fold more potent than CP-456,773 in the human whole blood assay, the most relevant for predicting human efficacy. These esters are highly differentiated from other literature NLRP3 inhibitors and have the potential for further optimisation.
  • ||||||||||  Review, Journal:  RNA Sensing of Mycobacterium tuberculosis and Its Impact on TB Vaccination Strategies. (Pubmed Central) -  Feb 10, 2020   
    The novel findings described here may change our current understanding of the host response to MTB and potentially impact clinical research, as well as future vaccination design. In this review, the current state of the art is summarized, and an outlook is given on how progress can be made.
  • ||||||||||  Tamoxis (tamoxifen) / Bioprofarma, eplerenone / Generic mfg.
    Journal:  Role of Angiogenesis and Chronic Inflammation in Fat Hypertrophy in NASH Pathology (Pubmed Central) -  Feb 8, 2020   
    The selective mineralocorticoid receptor (MR) inhibitor eplerenone (Ep) suppresses chronic inflammation in fat and the liver, improves glucose and lipid metabolism, and inhibits body weight and fat mass gain in mice fed a high-fat diet...Thus, we propose novel therapeutic approaches to NASH. Inhibition of PDGF receptor-β signaling prevents AT hypertrophy by regulating AT angiogenesis, and MR inhibitors directly suppress chronic inflammation in the AT and liver.
  • ||||||||||  Journal:  The NLRP3 inflammasome is involved with the pathogenesis of Mayaro virus. (Pubmed Central) -  Feb 8, 2020   
    In vivo infections performed in inflammasome-deficient mice indicate that NLRP3 is involved with footpad swelling, inflammation and pain, establishing a role of the NLRP3 inflammasome in the MAYV pathogenesis. Accordingly, we detected higher levels of caspase1-p20, IL-1β and IL-18 in the serum of MAYV-infected patients as compared to healthy individuals, supporting the participation of the NLRP3-inflammasome during MAYV infection in humans.
  • ||||||||||  Journal:  Structural mechanism for NEK7-licensed activation of NLRP3 inflammasome. (Pubmed Central) -  Feb 7, 2020   
    Mutations to this interface abolish the ability of NEK7 or NLRP3 to rescue NLRP3 activation in NEK7-knockout or NLRP3-knockout cells. These data suggest that NEK7 bridges adjacent NLRP3 subunits with bipartite interactions to mediate the activation of the NLRP3 inflammasome.
  • ||||||||||  Journal:  Melatonin prevents sepsis-induced renal injury via the PINK1/Parkin1 signaling pathway. (Pubmed Central) -  Feb 7, 2020   
    Finally, the apoptotic rate was found to be the highest in the CLP group and the lowest in the sham group. Taken together, in evaluating the therapeutic effect of MT on sepsis‑induced renal injury, the results of the present study showed that MT alleviated sepsis‑induced renal injury by regulating the expression of PINK1, Parkin1, NLRP3, ASC and cleaved caspase‑1 in rats.
  • ||||||||||  bleomycin / Generic mfg., BMS
    Journal:  HIF‑1α promotes NLRP3 inflammasome activation in bleomycin‑induced acute lung injury. (Pubmed Central) -  Feb 7, 2020   
    Therefore, the present study indicated that HIF‑1α could modulate the activation of the NLRP3 inflammasome and the secretion of IL‑1β through NF‑κB signaling in BLM‑induced ALI. The current results improve understanding of the mechanism of ALI and may provide new ideas for identifying therapeutic targets of ALI.