NLRP3 inhib 
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  • ||||||||||  Journal:  Cynarin suppresses gouty arthritis induced by monosodium urate crystals. (Pubmed Central) -  May 22, 2022   
    Cyn treatment reduced hind paw swelling and M1 macrophage infiltration, suppressed the mRNA expression of inflammatory factors, and inhibited NLRP3 inflammasome activation in vivo, in addition to inhibiting the phosphorylation of IKKa/β, p65, and c-Jun NH 2-terminal kinase (JNK). Furthermore, Cyn exerted anti-inflammatory and anti-swelling effects in mice with GA by regulating the NF-κB and JNK pathways and NLRP3 inflammasomes.
  • ||||||||||  desipramine / Generic mfg.
    Journal:  The interplay between ASMase signaling pathway and NLRP3 in the epithelial to mesenchymal transition of HBE cells induced by silica. (Pubmed Central) -  May 20, 2022   
    The ASMase inhibitor desipramine decreased the level of S1P and the expression of α-smooth muscle actin (α-SMA) and NLRP3 in SiO dust-stained HBE cells, whereas the expression of E-cadherin (E-cad) increased...Inhibition of ASMase activity or NLRP3 expression reduced the SiO dust-induced cell inflammatory response and slowed the occurrence of EMT in HBE cells. Therefore, NLRP3 and ASMase may interact in SiO dust-induced EMT in HBE cells.
  • ||||||||||  Zyclara (imiquimod) / Mochida, Viatris, Bausch Health
    Journal:  Ginsenoside Rg1 ameliorates psoriasis-like skin lesions by suppressing proliferation and NLRP3 inflammasomes in keratinocytes. (Pubmed Central) -  May 20, 2022   
    PRACTICAL APPLICATIONS: This is the very first study to explore the efficacy of ginsenoside Rg1 against psoriasis-like skin lesions to reveal the underlying mechanism. In this paper, the detection of skin histopathological analysis, CCK-8, flow cytometry, western blot, and ELISA analysis shows that ginsenoside Rg1 has preventive effect on psoriasis caused by imiquimod or M5 cocktail through inhibiting NLRP3 inflammasome, which helps in the development of novel nutraceutical/functional food against psoriasis and thus could improve the quality of life in psoriasis patients.
  • ||||||||||  Preclinical, Journal:  Ambient particulate matter exposure plus a high-fat diet exacerbate renal injury by activating the NLRP3 inflammasome and TGF-β1/Smad2 signaling pathway in mice. (Pubmed Central) -  May 20, 2022   
    In this paper, the detection of skin histopathological analysis, CCK-8, flow cytometry, western blot, and ELISA analysis shows that ginsenoside Rg1 has preventive effect on psoriasis caused by imiquimod or M5 cocktail through inhibiting NLRP3 inflammasome, which helps in the development of novel nutraceutical/functional food against psoriasis and thus could improve the quality of life in psoriasis patients. Taken together, our data indicated that PM exposure caused renal inflammation and induced profibrotic effects on the kidney, and combined exposure to ambient PM and a HFD exacerbated renal injury, which may involve activation of the NLRP3 inflammasome and the TGF-β1/Smad2 signaling pathway.
  • ||||||||||  Journal:  Ketogenic diet ameliorates inflammation by inhibiting the NLRP3 inflammasome in osteoarthritis. (Pubmed Central) -  May 20, 2022   
    Taken together, our data indicated that PM exposure caused renal inflammation and induced profibrotic effects on the kidney, and combined exposure to ambient PM and a HFD exacerbated renal injury, which may involve activation of the NLRP3 inflammasome and the TGF-β1/Smad2 signaling pathway. KD can protect the articular cartilage and subchondral bone in a rat OA model by inhibiting NLRP3 inflammasome activation and reducing the OA inflammatory response.
  • ||||||||||  nitroglycerin / Generic mfg.
    Preclinical, Journal:  Effect of BAY-117082, a NLRP3 inflammasome inhibitor, in a mouse model of nitroglycerin (NTG)-induced migraine. (Pubmed Central) -  May 14, 2022   
    Additionally, the treatment with BAY-117082 at doses of 5 mg/kg and 10 mg/kg significantly modulated p-ERK/p-CREB axis activation through the reduction of p-ERK, p-AKT, p-CREB and p-PI3K expression. Therefore, the obtained results offer new insight into the role of NLRP3 inflammasome pathway and p-ERK/p-CREB axis in migraine pathogenesis, suggesting that BAY-117082 could be considered a novel therapeutic strategy to treat migraine.
  • ||||||||||  Journal:  Mechanistic Insights of Sulfonamide-Based NLRP3 Inhibitors for the Treatment of Neurodegenerative Diseases. (Pubmed Central) -  May 14, 2022   
    Using our chemical probe in a pull-down assay, we also discovered other potential targets within the inflammasome pathway, including a protein that was recently termed "undruggable". These results suggest a novel mechanism of inhibition by our compounds and further studies are currently underway to improve these inhibitors as potential therapeutics for neuroinflammation in neurodegenerative diseases.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Enhanced autophagy alleviated corneal allograft rejection via inhibiting NLRP3 inflammasome activity. (Pubmed Central) -  May 12, 2022   
    Here, we showed that rapamycin (RAPA)-induced autophagy alleviated corneal allograft rejection...Moreover, we further revealed that pharmacologically blocking NLRP3 inflammasome signaling prolonged the survival of corneal allografts. Taken together, these findings underscored the critical roles of enhanced autophagy in treating corneal allograft rejection, which provided an alternative intervention strategy to control corneal transplantation rejection.
  • ||||||||||  Journal:  SIRT1 alleviates IL-1β induced nucleus pulposus cells pyroptosis via mitophagy in intervertebral disc degeneration. (Pubmed Central) -  May 12, 2022   
    In vivo, SIRT1 agonist (SRT1720) treatment decreased the expression of NLRP3, p20, and IL-1β, increased the expression of PINK1 and LC3, delayed IVDD process in the rat model. Taken together, our results indicate that SIRT1 alleviates IL-1β induced NLRP3 inflammasome activation via mitophagy in NPCs, SIRT1 may be a potential therapeutic target to alleviate NLRP3- activated pyroptosis in the inflammatory stress related IVDD.
  • ||||||||||  belnacasan (VX-765) / Vertex
    Journal:  Tricalcium phosphate particles promote pyroptotic death of calvaria osteocytes through the ROS/NLRP3/Caspase-1 signaling axis in amouse osteolysis model. (Pubmed Central) -  May 12, 2022   
    In addition, TCP particles increased the levels of intracellular reactive oxygen species (ROS) and malonaldehyde (MDA), whereas decreased the antioxidant enzyme nuclear factor E2-related factor 2 (Nrf2) level, leading to oxidative stress in calvaria osteocytes; the ROS scavenger N-acetylcysteine (NAC) attenuated these effects of pyroptotic death and the NLPR3 activation triggered by TCP particles. Collectively, our data suggested that TCP particles promote pyroptotic death of calvaria osteocytes through the ROS/NLRP3/Caspase-1 signaling axis, contributing to osteoclastogenesis and periprosthetic osteolysis.
  • ||||||||||  Zanosar (streptozocin) / Teva
    Journal:  ManNAc protects against podocyte pyroptosis via inhibiting mitochondrial damage and ROS/NLRP3 signaling pathway in diabetic kidney injury model. (Pubmed Central) -  May 12, 2022   
    The male 8-week-old C57BL/6 mice were divided into three groups: control group, Streptozocin (STZ)-induced DN group, and ManNAc treated diabetic group...Further, ManNAc administration significantly alleviated podocyte pyroptosis through inhibiting ROS/NLRP3 signaling pathway. Therefore, these results elucidated that the upregulated expression of Angptl4 was involved in podocyte injury and ManNAc treatment protected against podocyte pyroptosis via inhibiting mitochondrial injury and ROS/NLRP3 signaling pathway in DN mice.
  • ||||||||||  Journal:  Inflammasome involvement in CS-induced damage in HaCaT keratinocytes. (Pubmed Central) -  May 12, 2022   
    Of note is that, while CS inhibited NLRP3 activation, it was able to activate NLRP1, leading to an increased secretion of the proinflammatory cytokines IL-1β and IL-18. This study highlights the importance of the inflammasome machinery in CS that more in general, in pollution, affects cutaneous tissues and the important cross-talk between different members of the NLRP inflammasome family.
  • ||||||||||  fasiglifam (TAK-875) / Takeda, thapsigargin / University of Nottingham, Pirbright Institute
    Inhibition of NLRP3 inflammasome by GPR40 agonists (Poster Area) -  May 12, 2022 - Abstract #EASLILC2022EASL_ILC_2054;    
    Pre-exposure of BMDM to TAK875 suppressed ATP-induced intracellular Ca2+ increase, which was reversed by thapsigargin, a sarco/ endoplasmic reticulum Ca2+-ATPase (SERCA) inhibitor. These findings provide an evidence that free fatty acidsensing GPR40 plays a key role in NLRP3 inflammasome pathway.
  • ||||||||||  Journal:  Hypobaric hypoxia triggers pyroptosis in the retina via NLRP3 inflammasome activation. (Pubmed Central) -  May 7, 2022   
    RAHC attenuates hypobaric hypoxia-triggered retinal pyroptosis via inhibiting NLRP3 inflammasome activation and release of pro-inflammatory cytokines. The involvement of pyroptosis pathway in the retina in response to hypobaric hypoxia supports a novel insight to clarify the pathogenesis of hypobaric hypoxia-induced retinal impairment and provides a feasibility of inflammasome modulation for preserving retinal function.
  • ||||||||||  glibenclamide / Generic mfg.
    Journal:  Glibenclamide alleviates β adrenergic receptor activation-induced cardiac inflammation. (Pubmed Central) -  May 6, 2022   
    In conclusion, glibenclamide alleviates β-AR overactivation-induced cardiac inflammation by inhibiting the NLRP3 inflammasome. The underlying mechanism involves glibenclamide-mediated suppression of potassium efflux and ROS generation by inhibiting the cAMP/PKA pathway.
  • ||||||||||  emricasan (IDN 6556) / Histogen, Amerimmune
    Journal:  Gout-associated monosodium urate crystal-induced necrosis is independent of NLRP3 activity but can be suppressed by combined inhibitors for multiple signaling pathways. (Pubmed Central) -  May 6, 2022   
    Moreover, a triple combination of GSK'872, GW806742X, and IDN-6556 (pan-caspase inhibitor) displayed enhanced inhibition of the necrosis, which was further fortified by the addition of MCC950 (NLRP3 inhibitor), suggesting that multiple cell death pathways might have been triggered by MSU crystals...Besides, baicalin gavage significantly ameliorated MSU crystal-induced peritonitis in mice. Altogether, our data indicate that MSU crystals induce NLRP3-independent necrosis, which can be inhibited by combined inhibitors for multiple signaling pathways, highlighting a new avenue for the treatment of gouty arthritis.
  • ||||||||||  COG 133 / Cognosci, COG 112 / Cognosci
    Journal:  COG133 Attenuates the Early Brain Injury Induced by Blood-Brain Barrier Disruption in Experimental Subarachnoid Hemorrhage. (Pubmed Central) -  May 6, 2022   
    In terms of molecular mechanism, COG133 inhibits blood-brain barrier destruction through the proinflammatory CypA-NF-κB-MMP9 pathway and reduces neuronal pyroptosis by inhibiting NLRP3 inflammasome activation. In conclusion, this study demonstrated that apoE-mimetic peptide, COG133, can play a neuroprotective role by protecting blood-brain barrier function and inhibiting brain cell pyroptosis to reduce early brain injury after subarachnoid hemorrhage.
  • ||||||||||  Journal:  BAFF Blockade Attenuates DSS-Induced Chronic Colitis via Inhibiting NLRP3 Inflammasome and NF-κB Activation. (Pubmed Central) -  May 6, 2022   
    These results suggested that BAFF blockade protected against colitis partially by relieving inflammation, inhibiting intestinal NLRP3 inflammasome and NF-κB signaling pathway from macrophages. BAFF plays an important role in inflammation regulation in IBD, thus providing a novel idea for further research on colitis and experimental evidences for novel potential therapeutic target in IBD.
  • ||||||||||  Journal:  Extracellular vesicles derived from head and neck squamous cells carcinoma inhibit NLRP3 inflammasomes. (Pubmed Central) -  May 3, 2022   
    In fact, HNSCC-derived VSF inhibited the induction of pro-IL-1β and pro-caspase-1 proteins and NLRP3 gene expression during the priming phase of inflammasome activation. Thus, our findings contribute to a better understanding of how tumor-derived EVs modulate inflammatory response by demonstrating their role in inhibiting NLRP3 inflammasomes.