NLRP3 inhib 
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  • ||||||||||  Journal:  The Immunomodulatory Metabolite Itaconate Modifies NLRP3 and Inhibits Inflammasome Activation. (Pubmed Central) -  Nov 10, 2021   
    Furthermore, 4-OI inhibited NLRP3-dependent IL-1β release from PBMCs isolated from cryopyrin-associated periodic syndrome (CAPS) patients, and reduced inflammation in an in vivo model of urate-induced peritonitis. Our results identify itaconate as an endogenous metabolic regulator of the NLRP3 inflammasome and describe a process that may be exploited therapeutically to alleviate inflammation in NLRP3-driven disorders.
  • ||||||||||  Journal:  Treatment With Melatonin After Corneal Graft Attenuates Rejection. (Pubmed Central) -  Nov 7, 2021   
    Our study demonstrates that MT promotes the survival of mouse corneal grafts by inhibiting NLRP3-mediated immune regulation, reducing immune cell activation and cell migration, and inhibiting the production of inflammatory-related cytokines. Treatment with MT might provide a potential clinical therapeutic target for corneal transplantation.
  • ||||||||||  Journal:  Antituberculosis Drugs (Rifampicin and Isoniazid) Induce Liver Injury by Regulating NLRP3 Inflammasomes. (Pubmed Central) -  Nov 6, 2021   
    The NLRP3 inflammasome was required for INH- and RIF-induced liver injuries that were produced by inflammatory responses, OS, the antioxidant defense system, and drug-metabolizing enzymes. This study indicated that the NLRP3 inflammasome is involved in antituberculosis drug-induced liver injuries (ATLIs) and suggests NLRP3 as a potential target for attenuating the inflammation response in ATLIs.
  • ||||||||||  Preclinical, Journal:  Vinpocetine attenuates ischemic stroke through inhibiting NLRP3 inflammasome expression in mice. (Pubmed Central) -  Nov 5, 2021   
    The experimental results indicated that post-treatment with Vinp decreased cerebral infarct size, improved behavior recover, reduced NLRP3 inflammasome expression, suppress the transfer of NF-κB to nucleus and pro-inflammatory cytokines release in MCAO/R mice. In conclusion, the present study demonstrates that Vinp alleviates ischemic stroke by regulating levels of NLRP3 inflammasome, NF-κB and pro-inflammatory cytokines in vivo, offering an alternative medication for ischemic stroke associated with inflammation.
  • ||||||||||  Preclinical, Journal:  Ochratoxin A induces nephrotoxicity in vitro and in vivo via pyroptosis. (Pubmed Central) -  Nov 5, 2021   
    Furthermore, knockdown of caspase-1 also ameliorated OTA-induced renal fibrosis via the inhibition of pyroptosis. Collectively, the chosen doses of OTA-triggered nephrotoxicity through NLRP3 inflammasome activation and caspase-1-dependent pyroptosis both in vitro and in vivo.
  • ||||||||||  Journal:  A phenotypic high-content, high-throughput screen identifies inhibitors of NLRP3 inflammasome activation. (Pubmed Central) -  Nov 5, 2021   
    Our high-content screening assay yielded robust assay metrics and identified a number of inhibitors of NLRP3-dependent ASC speck formation, including compounds targeting HSP90, JAK and IKK-β. Additional assays to investigate inflammasome priming or activation, NLRP3 downstream effectors such as caspase-1, IL-1β and pyroptosis form the basis of a screening cascade to identify NLRP3 inflammasome inhibitors in drug discovery programs.
  • ||||||||||  Journal, IO biomarker:  NLRP3 Triggers Attenuate Lipocalin-2 Expression Independent with Inflammasome Activation. (Pubmed Central) -  Oct 28, 2021   
    At the same time, no changes in the other cytokines and IκBζ, a well-known transcriptional factor of Lcn2 transcription, were observed. Overall, NLRP3 triggers are a regulator of LCN2 expression suggesting a new linkage of inflammasome activation and LCN2 secretion in the innate immunity.
  • ||||||||||  Review, Journal:  Mechanisms of Kidney Cell Pyroptosis in Chronic Kidney Disease and the Effects of Traditional Chinese Medicine. (Pubmed Central) -  Oct 25, 2021   
    Traditional Chinese medicine (TCM) and extracts can interfere with the occurrence and development of kidney cell pyroptosis in CKD by inhibiting the NLRP3 signaling pathway and oxidative stress, activating Nrf-2 signaling, protecting mitochondrial integrity, regulating AMPK signaling, and regulating TXNIP/NLRP3 axis, which have become increasingly prominent. It is critical to explore the effects of TCM on kidney cell pyroptosis in CKD and its mechanisms to identify targets and develop new and effective drugs.
  • ||||||||||  Journal:  CMPK2 accelerates liver ischemia/reperfusion injury via the NLRP3 signaling pathway. (Pubmed Central) -  Oct 22, 2021   
    In conclusion, the results of the present study demonstrate that CMPK2 is indispensable for NLRP3 inflammasome activation, making CMPK2 an effective target to relieve the liver from I/R injury. In addition, the function of CMPK2 is closely associated with NLRP3 inflammasome activation, instead of AIM2.
  • ||||||||||  dapansutrile (OLT1177) / Olatec Therap
    Journal, Myeloid-derived suppressor cells, PD(L)-1 Biomarker, IO biomarker:  Tumor NLRP3-Derived IL-1β Drives the IL-6/STAT3 Axis Resulting in Sustained MDSC-Mediated Immunosuppression. (Pubmed Central) -  Oct 22, 2021   
    In PMN-MDSCs isolated from tumor-bearing mice treated with OLT1177, we observed significant reductions in immunosuppressive genes such as Pdcd1l1, Arg1, Il10 and Tgfb1. In conclusion, the data presented here show that the inhibition of NLRP3 reduces IL-1β induction of pSTAT3(Y705) preventing expression of immunosuppressive genes as well as activity in PMN-MDSCs.
  • ||||||||||  Ilaris (canakinumab) / Novartis
    Journal:  Anti-inflammatory therapy in ischaemic heart disease: from canakinumab to colchicine. (Pubmed Central) -  Oct 20, 2021   
    In summary, canakinumab and colchicine have shown efficacy in preventing MACE in ischaemic heart disease patients, but only colchicine has acceptable safety (and cost) for use in secondary cardiovascular prevention. Clinical results are expected with the anti-IL6 ziltivekimab.
  • ||||||||||  bardoxolone methyl (RTA 402) / Kyowa Kirin, Reata
    [VIRTUAL] Nrf2 Activators Induce Inflammasome Attenuation: Possible Role in Diabetic Nephropathy () -  Oct 17, 2021 - Abstract #KIDNEYWEEK2021KIDNEY_WEEK_2008;    
    Mouse bone marrow macrophages were treated with Bardoxolone (1µM), an Nrf2 inducer, and ND-13 (1µM) for 24 hours...Compared to controls and diabetic individuals, patients with diabetic nephropathy presented a trend to increase IL-1β release. Conclusion All these data point out that inflammasome pre-activation could have a role in the pathogenesis of diabetic nephropathy, that Nrf2 pathway stimulation is a promising approach to decrease immune cells inflammasome pre-activation, and ND-13 could be a new approach to protect the renal damage associated to inflammasome over-activation in renal diseases.