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  • ||||||||||  Review, Journal:  A Spotlight on the Underlying Activation Mechanisms of the NLRP3 Inflammasome and its Role in Atherosclerosis: A Review. (Pubmed Central) -  Sep 23, 2021   
    Inflammasome-mediated signaling interference could decrease inflammation and mitigate illness severity. In this section, we provide an overview of the present literature on the underlying mechanisms leading to the activation of NLRP3 inflammasome and the role of NLRP3 inflammasome in the progression of atherogenesis and highlight the possibility of therapeutic interventions due to mechanisms involved in the of inhibition of NLRP3 activation.
  • ||||||||||  Preclinical, Journal:  Electroacupuncture Attenuates Liver Inflammation in Nonalcoholic Fatty Liver Disease Rats. (Pubmed Central) -  Sep 23, 2021   
    EA relieved liver injury in NAFLD rats, and its mechanism may be related to the regulation of Sirt1/NF-κB pathway in rats. This is the first report that electroacupuncture alleviates liver inflammatory reaction of nonalcoholic fatty liver by enhancing Sirt1 expression and inhibiting NLRP3/NF-kB signal pathway.
  • ||||||||||  Journal:  Flavonoids with Inhibitory Effects on NLRP3 Inflammasome Activation from Millettia velutina. (Pubmed Central) -  Sep 22, 2021   
    Most importantly, compound 6 exerted potent protective effects in the LPS-induced septic shock mice model by improving the survival rate of mice and suppressing serum IL-1β release. These results demonstrated that compound 6 had the potential to be developed as a broad-spectrum NLRP3 inflammasome inhibitor for the treatment of NLRP3-related disease.
  • ||||||||||  sapanisertib (TAK-228) / Takeda
    Journal:  Inhibition of NLRP3 Inflammasome Activation and Pyroptosis in Macrophages by Taraxasterol Is Associated With Its Regulation on mTOR Signaling. (Pubmed Central) -  Sep 19, 2021   
    Moreover, TAS treatment alleviated mitochondrial damage by nigericin and improved mouse survival from bacterial infection, accompanied by reduced IL-1β levels in vivo. Collectively, by inhibiting the NLRP3 inflammasome activation, TAS displayed anti-inflammatory effects likely through regulation of the mTOR signaling in macrophages, highlighting a potential action mechanism for the anti-inflammatory activity of Dandelion in treating inflammation-related disorders, which warrants further clinical investigation.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  Dopamine D1 receptor alleviates doxorubicin-induced cardiac injury by inhibiting NLRP3 inflammasome. (Pubmed Central) -  Sep 19, 2021   
    Moreover, application of A-68930 to activate DRD1 reduced cardiac injury and fibrosis in a DOX-treated mouse model by suppressing the NLRP3 inflammasome in the heart. These findings indicate that DRD1 signaling may protect against DOX-induced cardiac injury by inhibiting the NLRP3 inflammasome-mediated inflammation.
  • ||||||||||  Journal:  Icariin alleviates rheumatoid arthritis via regulating miR-223-3p/NLRP3 signalling axis. (Pubmed Central) -  Sep 17, 2021   
    Additionally, anti-RA activity of icariin was restored by NLRP3 inhibitor MCC950 in miR-223-3p knockdown RA-FLS cells. Icariin inhibits proliferation and inflammation, promotes apoptosis of RA-FLS cells by regulating miR-223-3p/NLRP3 signalling, which may serve as a potential therapeutic target to alleviate RA.
  • ||||||||||  fluoxetine / Generic mfg.
    Preclinical, Journal:  Menhaden fish oil attenuates postpartum depression in rat model via inhibition of NLRP3-inflammasome driven inflammatory pathway. (Pubmed Central) -  Sep 16, 2021   
    Thirty six virgin adult female rats (n = 6) were randomly divided into six groups; Group 1-3 were normal control (NC), Sham (SHAM) and ovariectomized group (OVX) respectively whereas group 4-6 were PPD rats forced-fed once daily with distilled water (PPD), fish oil (PPD + FO; 9 g/kg) and Fluoxetine (PPD + FLX; 15 mg/kg) respectively from postpartum day 1 and continued for 10 consecutive days...In conclusion, 10 days supplementation with FO ameliorated the depressive-like behaviors in PPD rats by targeting the NFкB/NLRP3/caspase-1/IL-1β activity. This has shed light on the potential of NLRP3 as a therapeutic target in treatment of PPD in rats.
  • ||||||||||  Journal:  Sensing soluble uric acid by Naip1-Nlrp3 platform. (Pubmed Central) -  Sep 15, 2021   
    Moreover, molecular interaction experiments showed that Naip1 directly recognizes sUA. Accordingly, Naip may be the sUA receptor lost through the human evolutionary process, and a better understanding of its recognition may lead to novel anti-hyperuricaemia therapies.
  • ||||||||||  Review, Journal:  NLRP3 Ubiquitination-A New Approach to Target NLRP3 Inflammasome Activation. (Pubmed Central) -  Sep 15, 2021   
    The regulation of ubiquitination and deubiquitination of NLRP3 has emerged as a potential therapeutic target for NLRP3 inflammasome-associated inflammatory disorders. In this review, we discuss the ubiquitination and deubiquitination system for NLRP3 inflammasome activation and the inhibitors that can be used as potential therapeutic agents to modulate the activation of the NLRP3 inflammasome.
  • ||||||||||  Journal:  Overexpression of Limb Bud and Heart Alleviates Sepsis-Induced Acute Lung Injury via Inhibiting the NLRP3 Inflammasome. (Pubmed Central) -  Sep 12, 2021   
    Moreover, MCC950 reversed the promoting effects of LBH silencing on proinflammatory cytokine expression and NLRP3 inflammasome activation in LPS-induced A549 cells. LBH alleviated lung injury in sepsis-induced ALI mouse model by inhibiting inflammation and NLRP3 inflammasome, and restrained the inflammation by inhibiting NLRP3 inflammasome in LPS-induced A549 cells, providing a novel therapeutic target for ALI.
  • ||||||||||  Kineret (anakinra) / SOBI, Arcalyst (rilonacept) / Regeneron, Kiniksa, Ilaris (canakinumab) / Novartis
    Preclinical, Review, Journal:  Promise of the NLRP3 Inflammasome Inhibitors in In Vivo Disease Models. (Pubmed Central) -  Sep 5, 2021   
    For instance, treatments that focus on systemically negating IL-1β (i.e., anakinra, rilonacept, and canakinumab) have been reported to result in an escalated peril of infections. Therefore, given the therapeutic promise of an NLRP3 inhibitor, the concerted escalated venture of the scientific sorority in the advancement of small molecules focusing on direct NLRP3 inflammasome inhibition is quite predictable.
  • ||||||||||  Bay11-7082 / InvivoGen
    Journal:  P2X7 Receptor Induces Pyroptotic Inflammation and Cartilage Degradation in Osteoarthritis via NF-κB/NLRP3 Crosstalk. (Pubmed Central) -  Sep 4, 2021   
    In this study, Sprague-Dawley rats were injected in the knee with monosodium iodoacetate (MIA) to induce OA, followed by multiple intra-articular injections with P2X7R antagonist A740003, P2X7R agonist BzATP, NF-κB inhibitor Bay 11-7082, and NLRP3 inhibitor CY-09...In conclusion, activated P2X7 promoted extracellular matrix degradation and pyroptotic inflammation in OA chondrocytes through NF-κB/NLRP3 crosstalk, thus, aggravating the symptoms of OA. The study findings suggest P2X7 as a potential target for inflammation treatment, providing new avenues for OA research and therapy.
  • ||||||||||  Journal:  Fisetin Inhibits NLRP3 Inflammasome by Suppressing TLR4/MD2-Mediated Mitochondrial ROS Production. (Pubmed Central) -  Aug 28, 2021   
    Treatment of an LPS/ATP-stimulated zebrafish model with fisetin aided the recovery of the impaired heart rate, decreased the recruitment of macrophage to the brain, and gradually downregulated the expression of inflammasome-related genes. These results indicated that fisetin inhibited the TLR4/MD2-mediated activation of NLRP3 inflammasome by eliminating damaged mitochondria in a p62-dependent manner.
  • ||||||||||  Journal:  Isoorientin Attenuated the Pyroptotic Hepatocyte Damage Induced by Benzo[a]pyrene via ROS/NF-κB/NLRP3/Caspase-1 Signaling Pathway. (Pubmed Central) -  Aug 28, 2021   
    Caspase-1 inhibitor (Z-VAD-FMK) inhibited the characteristic pyroptosis protein expressions of Caspase-1, GSDMD-N, IL-18, and IL-1β, showing that the classic pyroptosis pathway depending on Caspase-1 was caused by BaP in HL-7702 cells. Consistent with the effects of the NLRP3 inhibitor (MCC950), NF-κB inhibitor (PDTC), ROS, and mtROS inhibitor (NAC and Mito-TEMPO), Iso weakened the stimulatory effects of BaP on the levels of ROS, the nuclear localization of NF-κB, and the activation of NLRP3 inflammasome and the characteristic indices of pyroptosis, demonstrating that Iso could alleviate the BaP-induced pyroptotic hepatocytes injury through inhibiting the ROS/NF-κB/NLRP3/Caspase-1 signaling pathway, which provides a new perspective and strategy to prevent liver injury induced by BaP.
  • ||||||||||  Journal:  Luteolin inhibits NLRP3 inflammasome activation via blocking ASC oligomerization. (Pubmed Central) -  Aug 25, 2021   
    Luteolin inhibited the activation step of NLRP3 inflammasome by interfering with ASC oligomerization. Taken together, these findings suggest that luteolin supplementation may suppress NLRP3 induction and activation process and thus potentially would be protective against NLRP3-mediated inflammatory diseases.
  • ||||||||||  Journal:  TRIM28 SUMOylates and stabilizes NLRP3 to facilitate inflammasome activation. (Pubmed Central) -  Aug 25, 2021   
    Concordantly, Trim28 deficiency attenuates NLRP3 inflammasome activation both in vitro and in vivo. These data identify a mechanism by which SUMOylation controls the cellular NLRP3 level and inflammasome activation, and reveal correlations and interactions of NLRP3 SUMOylation and ubiquitination during inflammasome activation.
  • ||||||||||  Journal:  Discovery and characterization of small molecule inhibitors of NLRP3 and NLRC4 inflammasomes. (Pubmed Central) -  Aug 22, 2021   
    We also validated the active pharmacophore shared among all the NLRP3 inhibitors, and through computational docking, we clarify key structural features for compound positioning within the inflammasome ATP binding site. Our study sets the basis for rational design and optimization of inflammasome-targeting probes and drugs.