NLRP3 inhib 
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  • ||||||||||  Journal:  UK5099 Inhibits the NLRP3 Inflammasome Independently of its Long-Established Target Mitochondrial Pyruvate Carrier. (Pubmed Central) -  Sep 27, 2024   
    Importantly, structure modification reveals that the inhibitory activities of UK5099 on NLRP3 are unrelated to the existence of the activated double bond within the UK5099 molecule. Thus, this study uncovers a previously unknown molecular target for UK5099, which not only offers a new candidate for the treatment of NLRP3-driven diseases but also confounds its use as an MPC inhibitor in immunometabolism studies.
  • ||||||||||  Journal:  Irisin Prevents Cell Death in High Glucose via NLRP3 Inhibition. (Pubmed Central) -  Sep 26, 2024   
    We found the protective effect of irisin on apoptosis and pyroptosis was abolished by NLRP3 over-expression. Our data suggest that irisin protects CMECs against apoptosis and pyroptosis, at least in part, by inhibiting NLRP3 inflammasome.
  • ||||||||||  Review, Journal:  The NLRP3 inflammasome in allergic diseases: mechanisms and therapeutic implications. (Pubmed Central) -  Sep 26, 2024   
    As preliminarily demonstrated, specific NLRP3 inflammatory vesicle inhibitors play refectory roles in animal models of allergic diseases, and it is believed that specific NLRP3 inflammasome inhibitors may be potential therapeutic agents for allergic diseases. This review highlights the progress of research on the NLRP3 inflammasome in allergic diseases, explores its contribution to different types of allergic diseases, and identifies promising clinical targets for intervention.
  • ||||||||||  Journal:  Design, Synthesis, and Bioevaluation of Novel NLRP3 Inhibitor with IBD Immunotherapy from the Virtual Screen. (Pubmed Central) -  Sep 26, 2024   
    Crucially, with acceptable mouse pharmacokinetic profiles, Z48 demonstrated notable therapeutic efficacy in a mouse model of DSS-induced ulcerative colitis, while displaying no significant therapeutic impact on NLRP3KO mice. In conclusion, this study provided a promising NLRP3 inflammasome inhibitor with novel molecular scaffold, poised for further development as a therapeutic candidate in the treatment of inflammatory bowel disease.
  • ||||||||||  NLRP3 Inflammasome Promotes Release of Peptidyl Arginine Deiminases2 and 4 from Human Neutrophils (In Person) -  Sep 25, 2024 - Abstract #ACRConvergence2024ACR_Convergence_1807;    
    We demonstrated cell death-independent release of PAD2 and PAD4 and identified NLRP3 inflammasome activation as a trigger promoting PAD release in human whole blood and neutrophils. Our data further suggest a role for NLRP3 inflammasome in amplifying the autoimmune response in RA.
  • ||||||||||  Journal:  Yang-Gan-Jiang-Mei formula alleviates non-alcoholic steatohepatitis by inhibiting NLRP3 inflammasome through mitophagy. (Pubmed Central) -  Sep 24, 2024   
    In addition, YGJM formula exhibited the promotion of PINK1/parkin-mediated mitophagy, which could perturb NLRP3 inflammasome activation, and as a result, the hepatocyte inflammation was also suppressed both in vitro and in vivo. Our preliminary results indicate that YGJM formula can ameliorate NASH mechanistically by interfering with PINK1/parkin-mediated mitophagy and NLRP3 inflammasome to exert anti-inflammation ability and promote mitochondrial function restoration.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  MIF aggravates experimental autoimmune prostatitis through activation of the NLRP3 inflammasome via the PI3K/AKT pathway. (Pubmed Central) -  Sep 17, 2024   
    Pharmacological inhibition of the PI3K/AKT pathway by LY294002 substantially reduced prostatic inflammation and macrophage infiltration, potentially by inhibiting NLRP3 inflammasome activation. These findings collectively suggest that MIF is a potential diagnostic marker for CNP and suggest that targeting MIF or its downstream signalling pathways, PI3K/AKT and NLRP3, might represent a novel therapeutic strategy for this condition.
  • ||||||||||  Tenelia (teneligliptin) / Daiichi Sankyo, Mitsubishi Tanabe
    Journal:  Macrophage modulation with dipeptidyl peptidase-4 inhibitors: A new frontier for treating diabetic cardiomyopathy? (Pubmed Central) -  Sep 16, 2024   
    These compounds may achieve this by elevating glucagon-like peptide-1 levels and potentially inhibiting the NLRP3 inflammasome. Further studies on teneligliptin in combination with other therapies targeting different aspects of DCM could be suggested for developing more effective treatment strategies to improve cardiovascular health in diabetic patients.
  • ||||||||||  Bosulif (bosutinib) / Pfizer, Iclusig (ponatinib) / Takeda, Otsuka, Tasigna (nilotinib) / Novartis, Inhibikase
    Journal:  Investigation of the Role of NLRP3 Inflammasome Activation in New-Generation BCR-ABL1 Tyrosine Kinase Inhibitors-Induced Hepatotoxicity. (Pubmed Central) -  Sep 15, 2024   
    Indeed, bosutinib and nilotinib were associated with severe hepatotoxicity compared with imatinib...This study aimed to investigate the role of NLRP3 inflammasome activation in the underlying mechanism of ponatinib and bosutinib-induced hepatotoxicity...In summary, NLRP3 inflammasome activation is involved in new-generation BCR-ABL1 TKIs-triggered hepatotoxicity. Mitochondrial damage and reactive oxygen species accumulation were significant upstream signaling events in this signaling pathway.
  • ||||||||||  Journal:  Kynurenine Attenuates Ulcerative Colitis Mediated by the Aryl Hydrocarbon Receptor. (Pubmed Central) -  Sep 14, 2024   
    KYN could trigger AhR activation, inactivate the NF-?B signaling pathway, and inhibit NLRP3 inflammasome production, thus alleviating intestinal epithelial barrier dysfunction and reducing intestinal inflammation. In conclusion, the present study reveals that KYN ameliorates UC by improving the intestinal epithelial barrier and activating the AhR-NF-?B-NLRP3 signaling pathway, and it can be a promising therapeutic agent and dietary supplement for alleviating UC.
  • ||||||||||  Review, Journal:  Recent advances in the treatment of gout with NLRP3 inflammasome inhibitors. (Pubmed Central) -  Sep 11, 2024   
    In recent years, there has been significant academic and industrial interest in the development of NLRP3-targeted small molecule inhibitors as a promising therapeutic approach for gout. To assess the advancements in NLRP3 inflammasome inhibitors for gout treatment, this review offers a comprehensive analysis and evaluation of current clinical candidates and other inhibitors targeting NLRP3 inflammasome from a chemical structure standpoint, with the goal of identifying more efficacious options for clinical management of gout.
  • ||||||||||  Journal:  ?-Caryophyllene mitigates ischemic stroke-induced white matter lesions by inhibiting pyroptosis. (Pubmed Central) -  Sep 10, 2024   
    In addition, nigericin significantly exacerbates neurological outcomes and increases white matter lesions following BCP treatment in middle cerebral artery occlusion (MCAO) mice. These results suggest that BCP may ameliorate neurological deficits and white matter damage induced by cerebral ischemia through inhibiting NLRP3-mediated pyroptosis.