NLRP3 inhib 
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  • ||||||||||  dexmedetomidine / Generic mfg.
    Preclinical, Journal:  Dexmedetomidine's protective mechanism against hyperoxic injury in neonatal rats. (Pubmed Central) -  Jul 23, 2024   
    Furthermore, the expressions of pyroptosis-related proteins such as NLRP3, ASC, cleaved-caspase-1, and GSDMD were significantly decreased, along with the expressions of inflammatory factors in lung tissues. By inhibiting the NLRP3/caspase-1/GSDMD pyroptosis pathway, dexmedetomidine reduces the activation and release of inflammatory factors and provides a protective effect against hyperoxic lung injury in neonatal mice.
  • ||||||||||  Journal:  MLKL deficiency alleviates acute alcoholic liver injury via inhibition of NLRP3 inflammasome. (Pubmed Central) -  Jul 22, 2024   
    Mechanistically, inhibiting the nuclear translocation of MLKL reduced the nuclear entry of p65, the principal transcriptional regulator of NLRP3, thereby limiting the transcription of Nlrp3 mRNA and subsequent NLRP3 expression. Overall, this study unveils a novel mechanism of MLKL regulates the activation of NLRP3 inflammasomes in a necroptosis independant way in acute alcoholic liver injury.
  • ||||||||||  Journal:  Characterization of a small molecule inhibitor of the NLRP3 inflammasome and its potential use for acute lung injury. (Pubmed Central) -  Jul 20, 2024   
    Further studies of MS-II-124 in mouse model of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) and NLRP3 knockout mice demonstrated its target engagement, efficacy to suppress inflammatory cytokines and infiltration of immune cells in the lung tissues. In summary, the results support the therapeutic potential of MS-II-124 as a NLRP3 inhibitor and warrant future studies of this compound and its analogs to develop therapeutics for ALI/ARDS.
  • ||||||||||  Journal:  Gut microbiota-mediated activation of GSDMD ignites colorectal tumorigenesis. (Pubmed Central) -  Jul 18, 2024   
    Activation of GSDMD is also accompanied by the aggregation of the endosomal sorting complex required for transport (ESCRT) membrane repair proteins on the membrane of colorectal tumor cells, suggesting that active membrane repairment may prevent pyroptosis induced by the formation of GSDMD pore in tumor cells. Our results show that gut microbiota/NLRP3-mediated activation of GSDMD promotes the development of colorectal tumors, and supports the use of NLRP3 inhibitors to treat colon cancer.
  • ||||||||||  Repetitive transcranial magnetic stimulation relieves neuropathic pain by blocking integrin ?v?3 (Exhibition Hall/Poster Area) -  Jul 18, 2024 - Abstract #IASP2024IASP_954;    
    We identify a potential link between amygdala neural activity and integrin ?v?3, unveil a significant interaction between integrin ?v?3 and P2X7R in the amygdala, suggesting their involvement in the response to rTMS treatment. Further investigation into P2X7R downstream signaling pathways reveals the activation of the NLRP3 inflammatory signaling pathway as an intrinsic mechanism underlying rTMS efficacy.
  • ||||||||||  Journal:  Biflavonoid Methylchamaejasmin and Khaya grandifoliola (Pubmed Central) -  Jul 16, 2024   
    phagocytosis showed that M8 and KG pretreatments can restore the phagocytic activity of THP-1 cells, which was impaired following inflammasome activation. Altogether, our findings describe for the first time a promising role of biflavonoids and KG extract in preventing inflammasome activation and protecting against neuroinflammation, a key factor in AD development.
  • ||||||||||  Bay11-7082 / Bayer, belnacasan (VX-765) / Vertex
    Journal:  Enhanced Cardiomyocyte NLRP3 Inflammasome-Mediated Pyroptosis Promotes d-Galactose-Induced Cardiac Aging. (Pubmed Central) -  Jul 16, 2024   
    Altogether, our findings describe for the first time a promising role of biflavonoids and KG extract in preventing inflammasome activation and protecting against neuroinflammation, a key factor in AD development. The reactive oxygen species/nuclear factor ?-light-chain enhancer of activated B cells/NLRP3 signaling pathway loop contributes to d-galactose-treated cardiomyocyte senescence and cardiac aging.
  • ||||||||||  Journal:  Co-exposure of microcystin-LR and nitrite induced kidney injury through TLR4/NLRP3/GSDMD-mediated pyroptosis. (Pubmed Central) -  Jul 14, 2024   
    These findings provide compelling evidence that MC-LR combined with nitrite synergistically induces pyroptosis in the kidney by activating the TLR4/NLRP3/GSDMD pathway. Overall, this study significantly enhances our comprehension of how environmental toxins interact and induce harm to the kidneys, offering promising avenues for identifying therapeutic targets to alleviate their toxic effects on renal health.
  • ||||||||||  Tudcabil (tauroursodeoxycholic acid) / Bruschettini
    Journal:  Promoting longevity in aged liver through NLRP3 inflammasome inhibition using tauroursodeoxycholic acid (TUDCA) and SCD probiotics. (Pubmed Central) -  Jul 11, 2024   
    These results underscore the therapeutic potential of TUDCA and SCD Probiotics for managing age-associated liver disorders, illustrating their individual and synergistic effects on liver health and pathology. This study provides insights into the complex interactions of these agents, advocating for customized therapeutic approaches to combat liver fibrosis, enhance liver functionality, and decrease inflammation in aging populations.
  • ||||||||||  Journal:  Oridonin attenuates liver ischemia-reperfusion injury by suppressing PKM2/NLRP3-mediated macrophage pyroptosis. (Pubmed Central) -  Jul 11, 2024   
    This study provides insights into the complex interactions of these agents, advocating for customized therapeutic approaches to combat liver fibrosis, enhance liver functionality, and decrease inflammation in aging populations. Ori exerted protective effects on liver IRI via suppressing PKM2/NLRP3-mediated liver macrophage pyroptosis, which might become a potential therapeutic target in the clinic.
  • ||||||||||  Review, Journal:  Ketone body metabolism and the NLRP3 inflammasome in Alzheimer's disease. (Pubmed Central) -  Jul 11, 2024   
    Here, we review the role of the NLRP3 inflammasome and microglial ketone body metabolism in AD pathogenesis. We also highlight NLRP3 inflammasome inhibition by several ketone body therapies as a promising new treatment strategy for AD.
  • ||||||||||  Journal:  The critical role of NLRP3 inflammasome activation in Streptococcus suis-induced blood-brain barrier disruption. (Pubmed Central) -  Jul 10, 2024   
    In addition, the integrity of the BBB was protected with increased TJ proteins expression and decreased pathological injury after the inhibition of NLRP3 inflammasome, indicating NLRP3 inflammasome plays a destructive role in meningitis induced by S. suis. Our study expands the understanding on the role of NLRP3 inflammasome in bacterial meningitis, which provide the valuable information for the development of anti-infective agents targeting NLRP3 to treat bacterial meningitis.
  • ||||||||||  Journal:  Lyssavirus matrix protein inhibits NLRP3 inflammasome assembly by binding to NLRP3. (Pubmed Central) -  Jul 10, 2024   
    (IL-1?) production in bone-marrow-derived dendritic cells (BMDCs) to facilitate lyssavirus invasion into the brain thereby elevating pathogenicity in mice. Taken together, this study reveals a common mechanism by which lyssavirus inhibits NLRP3 inflammasome activation to evade host defenses.
  • ||||||||||  dapansutrile (OLT1177) / Olatec Therap
    Journal:  Dapansutrile OLT1177 suppresses foreign body response inflammation while preserving vascularisation of implanted materials. (Pubmed Central) -  Jul 8, 2024   
    Mechanistic studies revealed that this occurred through activation of early pro-angiogenic markers while suppressing late-stage anti-angiogenic markers. These findings establish OLT1177 as a promising therapeutic approach for mitigating implant fibrosis while supporting vascularisation, suggesting a highly promising selective immunosuppressive strategy for the FBR warranting further research to explore its optimal integration into medical materials and devices.
  • ||||||||||  Review, Journal:  The NLRP3 inflammasome in burns: a novel potential therapeutic target. (Pubmed Central) -  Jul 3, 2024   
    A better understanding of the pathophysiological mechanism underlying the healing of burn wounds may help find optimal therapeutic targets to promote the healing of burn wounds, reduce complications/sequelae following burn, and maximize the restoration of structure and function of burn skin. This review aimed to summarize current understanding of the roles and regulatory mechanisms of the NLRP3 inflammasome in burn wound healing, as well as the preclinical studies of the involvement of NLRP3 inhibitors in burn treatment, highlighting the potential application of NLRP3-targeted therapy in burn wounds.
  • ||||||||||  glibenclamide / Generic mfg.
    Journal:  Can Urinary Bladder Innervation Be Restored After Outlet Obstruction and Denervation? (Pubmed Central) -  Jul 3, 2024   
    It is unclear whether Cox-2 is involved in the decreased nerve density following obstruction, but Cox-2 mRNA increases 5-fold in obstructed bladder. Future therapy against bladder underactivity remaining following relief of obstruction includes either systemic treatment, perhaps by anti-inflammatory drugs, or local treatment by injection of stem cells, mature ganglion cells, and/or neurotrophins or neurotrimin into the bladder wall.
  • ||||||||||  OMT-28 / OMEICOS
    Journal:  Cardioprotective properties of OMT-28, a synthetic analog of omega-3 epoxyeicosanoids. (Pubmed Central) -  Jul 2, 2024   
    Furthermore, OMT-28 (1 ?M) limited IR-induced NLRP3 inflammasome activation similarly like a direct NLRP3 inhibitor (MCC950). Overall, this study demonstrates that OMT-28 possesses potent cardio-protective and anti-inflammatory properties supporting the hypothesis that extending the bioavailability of omega-3 epoxyeicosanoids may improve their prospects as therapeutic agents.
  • ||||||||||  Journal:  Three Undescribed Protoilludane-type Sesquiterpene Aryl Esters from (Pubmed Central) -  Jul 1, 2024   
    Based on electronic circular dichroism (ECD) calculations, the absolute configurations of three new compounds (1-3) were determined. The anti-inflammatory activity of compounds 1-10 was screened and compound 3 could dose-dependently decrease the level of lactate dehydrogenase, showing IC50 value of 4.525 ?M.
  • ||||||||||  Preclinical, Journal:  Roundup (Pubmed Central) -  Jun 24, 2024   
    In summary, our findings indicated that the premature senescence of granulosa cells caused by mitochondrial ROS-triggered NLRP3 inflammasome activation might contribute to the ovarian toxicity of Roundup, in addition to its known effects on steroidogenesis and apoptosis. The online version contains supplementary material available at 10.1007/s43188-024-00229-0.
  • ||||||||||  Journal:  A novel mechanism of resveratrol alleviates Toxoplasma gondii infection-induced pulmonary inflammation via inhibiting inflammasome activation. (Pubmed Central) -  Jun 23, 2024   
    Considering insights from previous research alongside the outcomes of the current investigation, it appears that the TLR4/NF-?B/NLRP3 signaling pathway emerges as a promising target for immunomodulation to alleviate lung injury from T. gondii infection. The evidence gathered in this study lays the groundwork for the continued exploration and potential future clinical deployment of RSV as a therapeutic agent with anti-Toxoplasma properties and the capability to modulate the inflammatory response.
  • ||||||||||  Journal:  Tryptanthrin suppresses multiple inflammasome activation to regulate NASH progression by targeting ASC protein. (Pubmed Central) -  Jun 23, 2024   
    The evidence gathered in this study lays the groundwork for the continued exploration and potential future clinical deployment of RSV as a therapeutic agent with anti-Toxoplasma properties and the capability to modulate the inflammatory response. In general, the requirement for ASC in multiple inflammasome complexes makes TPR, as a novel broad-spectrum inflammasome inhibitor, potentially useful for treating a wide range of multifactorial inflammasome-related diseases.