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- | Journal: STUB1 is acetylated by KAT5 and alleviates myocardial ischemia-reperfusion injury through LATS2-YAP-?-catenin axis. (Pubmed Central) - Apr 5, 2024
Notably, the inhibitory effect of STUB1 overexpression on cardiomyocyte pyroptosis was abolished by LATS2 overexpression or KAT5 depletion. Our findings suggest that KAT5 overexpression inhibits NLRP3-mediated cardiomyocyte pyroptosis to relieve MIRI through modulation of STUB1/LATS2/YAP/?-catenin axis, providing a potential therapeutic target for MIRI.
- Platycodon D protects human nasal epithelial cells from pyroptosis through the Nrf2/HO-1/ROS signaling cascade in chronic rhinosinusitis (Bilbao) - Apr 5, 2024 - Abstract #EAACI2024EAACI_802;
PLD inhibits NLRP3-mediated pyroptosis, preventing inflammatory damage in HNEpCs of patients with CRS by activating the Nrf2/HO-1 antioxidant signaling pathway. It in turn reduces ROS production and ameliorates mitochondrial damage.
- | clodronate disodium / Generic mfg.
Journal, Immunomodulating: Immunomodulation in allergic rhinitis: Insights from Th2 cells and NLRP3/IL-18 (Pubmed Central) - Apr 4, 2024
Manipulations using NLRP3-/-, ASC-/- mice, clodronate liposome treatment, and NLRP3 inhibitor MCC950 were performed to assess their impact on AR symptoms and immune responses...This comprehensive study unravels the pivotal role of NLRP3-mediated immune modulation and macrophage pyroptosis in Th1/Th2 balance regulation in OVA-induced AR. Targeting NLRP3 pathways with MCC950 emerged as a promising strategy to alleviate AR symptoms, providing insights for potential therapeutic interventions in AR management.
- | atorvastatin / Generic mfg.
Preclinical, Journal: Astragaloside IV attenuates renal tubule injury in DKD rats via suppression of CD36-mediated NLRP3 inflammasome activation. (Pubmed Central) - Apr 4, 2024
secretion in PA-induced HK-2 cells. AS-IV alleviated renal tubule interstitial inflammation and tubule epithelial cell apoptosis in DKD rats by inhibiting CD36-mediated lipid accumulation and NLRP3 inflammasome activation.
- | doxorubicin hydrochloride / Generic mfg.
Journal, IO biomarker: Investigation of polysaccharide from Radix Aconiti Lateralis Preparata (Fuzi) cardio protective effect on doxorubicin-induced chronic cardiotoxicity. (Pubmed Central) - Apr 4, 2024
AS-IV alleviated renal tubule interstitial inflammation and tubule epithelial cell apoptosis in DKD rats by inhibiting CD36-mediated lipid accumulation and NLRP3 inflammasome activation. FPS can protect heart function and structure in DICC mice by inhibiting NLRP3 inflammasome-mediated pyroptosis and IL-6/STAT3 pathway-induced apoptosis.
- | Journal: Berberine inhibits NLRP3 inflammasome activation and proinflammatory macrophage M1 polarization to accelerate peripheral nerve regeneration. (Pubmed Central) - Apr 3, 2024
Furthermore, BBR significantly downregulated the expression of the NLRP3 inflammasome and its associated molecules in macrophages, thereby mitigating NLRP3 inflammasome activation-induced macrophage M1 polarization and inflammation. In summary, BBR's neuroprotective effects were concomitant with the suppression of inflammation after PNI, achieved through the inhibition of NLRP3 inflammasome activation-induced macrophage M1 polarization.
- | Journal: Identification of a short sequence motif in the influenza A virus pathogenicity factor PB1-F2 required for inhibition of human NLRP3. (Pubmed Central) - Apr 3, 2024
Here, we demonstrate how this short peptide binds to NLRP3 and provide evidence that a four amino acid stretch in PB1-F2 is necessary and sufficient to mediate this binding. Our data identify a new virus-host interface required to block one signaling path of the innate host response against influenza A virus.
- | disulfiram / Generic mfg.
Journal: Disulfiram Improves Fat Graft Retention by Modulating Macrophage Polarization Via Inhibition of NLRP3 Inflammasome-Mediated Pyroptosis. (Pubmed Central) - Apr 3, 2024
Our results suggested that pyroptosis plays a crucial role in the inflammatory cascade within fat grafts. DSF, being a clinically available drug could be translated into a clinically effective drug for improving fat graft survival via inhibiting macrophage pyroptosis, thereby inducing M2 macrophage polarization and promoting neovascularization.
- | Preclinical, Journal: CXCL13/CXCR5 promote chronic postsurgical pain and astrocyte activation in rats by targeting NLRP3. (Pubmed Central) - Apr 3, 2024
The CXCL13/CXCR5 signaling could promote neuropathic pain, astrocytes activation, and NLRP3 inflammasome activation in CPSP model rats by targeting NLRP3. NLRP3 may be a potential target for the management of CPSP.
- ribavirin / Generic mfg.
Macrophage-augmented organoids recapitulate the complex pathophysiology of viral diseases affecting the liver and devise advanced treatment strategies (Poster Area) - Apr 2, 2024 - Abstract #EASLILC2024EASL_ILC_2205;
MaugOs support the productive infections of these three viruses, which in turn triggered inflammatory responses. MaugOs can capture the multi-dimensions of viral pathophysiology, and enable the development of advanced treatment strategies aiming at simultaneously targeting the virus and inflammation.
- | Votrient (pazopanib) / Novartis, BeiGene
Preclinical, Journal: Melatonin alleviates chronic stress-induced hippocampal microglia pyroptosis and subsequent depression-like behaviors by inhibiting Cathepsin B/NLRP3 signaling pathway in rats. (Pubmed Central) - Apr 1, 2024
Similarly, melatonin inhibited Cathepsin B agonist Pazopanib-induced activation of Cathepsin B/NLRP3 signaling pathway and HAPI cells pyroptosis...These results demonstrated that melatonin could alleviate CRS-induced hippocampal microglia pyroptosis by inhibiting Cathepsin B/NLRP3 signaling pathway, thereby improving depression-like behaviors in rats. This study reveals the molecular mechanism of melatonin in the prevention and treatment of chronic stress-related encephalopathy.
- | Journal, Myeloid-derived suppressor cells: MDSC-targeting gold nanoparticles enhance PD-1 tumor immunotherapy by inhibiting NLRP3 inflammasomes. (Pubmed Central) - Apr 1, 2024
Our findings unraveled a novel approach wherein peptide-modified Au NPs relieved the suppressive impact of the tumor microenvironment by inhibiting MDSCs-mediated IL-1? release, which is the first time reported the employing a nanostrategy at modulating MDSCs to reverse the immunosuppressive microenvironment and may hold promise as a potential therapeutic agent for cancer immunotherapy.
- | dexamethasone / Generic mfg.
Journal: Mahuang Fuzi Xixin decoction alleviates allergic rhinitis by inhibiting NLRP3/caspase-1/GSDMD-N-mediated pyroptosis. (Pubmed Central) - Apr 1, 2024
MFXD suppressed nasal epithelial pyroptosis by inhibiting the NLRP3/Caspase-1/GSDMD-N signaling pathway, which alleviates AR. Our results offer valuable insights into potential AR therapies and provide evidence for the clinical utilization of MFXD to treat AR.
- Discovery of clinical candidate GS8-164, a highly potent oral NLRP3 inflammasome inhibitor for inflammation disorders (Exhibit Hall F1; Poster Board Number: B522) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_2181;
In 14-day rat and dog toxicology studies, GS8-164 displayed good tolerance, excellent PK profile and a good safety window (>50 fold). GS8-164 is under IND-enabling study and the clinical development is planned towards early 2025.
- Aryl hydrocarbon receptor confers protection against macrophage pyroptosis and intestinal inflammation through regulating polyamine biosynthesis (Exhibit Hall F1; Poster Board Number: B535) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_2172;
GS8-164 is under IND-enabling study and the clinical development is planned towards early 2025. These findings suggest a functional role for the AhR/ODC1/polyamine axis in maintain intestinal homeostasis.
- Blocking of NLRP3 inflammasome activity alleviates iron-induced adverse effects in murine models of colitis (Exhibit Hall F1; Poster Board Number: B581) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_2075;
Intriguingly, deficiency of NLRP3 in HfeKO mice (Hfe-Nlrp3-DKO) significantly protected them from IL-10R neutralization-induced colitis. In conclusion, our study demonstrates that excess iron could exacerbate inflammation during IBD and that BHB could be used as a therapeutic to mitigate iron-induced inflammation in IBD.
- Air pollution PM2.5 uptake by macrophages induces NLRP3 inflammasome-dependent IL1 (Exhibit Hall F1; Poster Board Number: B620) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1893;
In conclusion, our study demonstrates that excess iron could exacerbate inflammation during IBD and that BHB could be used as a therapeutic to mitigate iron-induced inflammation in IBD. Moreover, specific inhibition of superoxide anion production from mitochondrial respiratory Complex I, but not III, blunted IL1
- Loss of myeloid-KLF2 mediates LPS-induced mortality in neonatal pups by NLRP3 inflammasome signaling and altered neutrophil aging (Exhibit Hall F1; Poster Board Number: B231) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1862;
It accelerates neutrophil aging, but leads to persistence of aged neutrophils in the circulation by reducing CXCR4 expression. Future mechanistic studies will focus on KLF2's regulation of NLRP3 and CXCR4 expression at P4 and P12.
- colchicine / Generic mfg.
Comprehensive evaluation of gout models for assessing drug efficacy: Insights from multifaceted approaches (Exhibit Hall F1; Poster Board Number: B862) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1450;
Various drugs, such as glucocorticoids, colchicine, and uric acid metabolic pathway-related drugs, were assessed for efficacy based on clinical phenotypes, cytokine profiling, histopathology, and measurement of peripheral blood uric acid levels.Distinct gout models exhibited unique characteristics in evaluating drug efficacy...Notably, NLRP3 inhibitors displayed a significant inhibitory effect on gout progression.This study provides critical insights into the selection of appropriate models and evaluation methods for assessing specific gout drug efficacy. Through a multifaceted comparison across diverse models, the research offers guidance for the development and clinical application of gout medications.
- M2-polarized macrophages prevent preterm birth and improve neonatal survival and immunity (Exhibit Hall F1; Poster Board Number: B595) - Mar 29, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_1197;
Our findings provide cogent evidence that M2 M? can serve as a cellular strategy to mitigate PTB and decrease neonatal mortality.
- | Journal: Chlojaponilactone B Attenuates THP-1 Macrophage Pyroptosis by Inhibiting the TLR/MyD88/NF-?B Pathway. (Pubmed Central) - Mar 28, 2024
Additionally, CJB suppressed LPS/ATP-induced elevations in TLRs, MyD88, pro-IL-1?, and NF-?B and blocked NF-?B p65 nuclear translocation. In summary, CJB inhibits NLRP3 activation and macrophage pyroptosis through the TLR/MyD88/NF-?B pathway, providing important evidence for its development as a potential drug for treating pyroptosis-related inflammatory diseases.
- | glibenclamide / Generic mfg.
Journal: Implications of NLRP3 Suppression Using Glibenclamide and miR-223 against Colorectal Cancer. (Pubmed Central) - Mar 28, 2024
Notably, neither gli nor WTmiR-223 effectively prevented sphere invasion. These data suggest that, while WTmiR-223 could have a better anticancer effect in CRC compared to gli, the sole usage of miR-223-mediated NLRP3 suppression may not be sufficient to prevent CRC metastasis.
- | Journal: Novel chemotype NLRP3 inhibitors that target the CRID3-binding pocket with high potency. (Pubmed Central) - Mar 27, 2024
These data suggest that, while WTmiR-223 could have a better anticancer effect in CRC compared to gli, the sole usage of miR-223-mediated NLRP3 suppression may not be sufficient to prevent CRC metastasis. NIC-12 selectively reduces circulating IL-1
- | hyoscine butylbromide oral / Generic mfg.
Journal: Design, Synthesis, and Biological Evaluation of Ferulic Acid Template-Based Novel Multifunctional Ligands Targeting NLRP3 Inflammasome for the Management of Alzheimer's Disease. (Pubmed Central) - Mar 25, 2024
Finally, 12o could reverse memory impairment in the scopolamine-induced AD mice model, as evident through in vivo and ex vivo studies. These findings suggest that this compound may act as a promising candidate for further improvement in the management of AD.
- | Journal: NLRP3/1-mediated pyroptosis: beneficial clues for the development of novel therapies for Alzheimer's disease. (Pubmed Central) - Mar 25, 2024
We also describe the structures of NLRP3 and NLRP1 and the role their activation plays in Alzheimer's disease. Finally, we examine the neuroprotective activity of small-molecule inhibitors, endogenous inhibitor proteins, microRNAs, and natural bioactive molecules that target NLRP3 and NLRP1, based on the rationale that inhibiting NLRP3 and NLRP1 inflammasome-mediated pyroptosis can be an effective therapeutic strategy for Alzheimer's disease.
- | Journal: Tolerogenic dendritic cells alleviate collagen-induced arthritis by regulating T-cell differentiation and inhibiting NLRP3-mediated apoptosis. (Pubmed Central) - Mar 25, 2024
Finally, we examine the neuroprotective activity of small-molecule inhibitors, endogenous inhibitor proteins, microRNAs, and natural bioactive molecules that target NLRP3 and NLRP1, based on the rationale that inhibiting NLRP3 and NLRP1 inflammasome-mediated pyroptosis can be an effective therapeutic strategy for Alzheimer's disease. Our findings underscore the efficacy of tolDCs in attenuating CIA progression through modulation of CD4+ T-cell subpopulations and inhibition of NLRP3-mediated pyroptosis.
- | Xpovio (selinexor) / Karyopharm, Menarini, FORUS Therap
Preclinical, Journal, IO biomarker: The XPO1 inhibitor selinexor ameliorates bleomycin-induced pulmonary fibrosis in mice via GBP5/NLRP3 inflammasome signaling. (Pubmed Central) - Mar 25, 2024
Taken together, our findings indicate that Sel ameliorates BLM-induced pulmonary fibrosis by targeting GBP5 via NLRP3 inflammasome signaling. Thus, the XPO1 inhibitor - Sel might be a potential therapeutic agent for pulmonary fibrosis.
- | Journal: Irisin protects against cardiac injury by inhibiting NLRP3 inflammasome-mediated pyroptosis during remodeling after infarction. (Pubmed Central) - Mar 25, 2024
Moreover, irisin was shown to significantly suppress the mRNA and protein expressions of key components involved in NLRP3 inflammasome pathway (NLRP3, ASC, caspase-1 (p20), and interleukin-18 (IL-18)) both in MI-induced mice and hypoxia/reoxygenation-treated cells. This study firstly reveals that the cardioprotective effect of irisin is mediated through the attenuation of NLRP3 inflammasome activation and pyroptosis, positioning irisin as a promising therapeutic agent for cardiac injury.
- | cyclophosphamide / Generic mfg.
Journal: ?-Ketoglutarate Improves Ovarian Reserve Function in Primary Ovarian Insufficiency by Inhibiting NLRP3-Mediated Pyroptosis of Granulosa Cells. (Pubmed Central) - Mar 25, 2024
This study firstly reveals that the cardioprotective effect of irisin is mediated through the attenuation of NLRP3 inflammasome activation and pyroptosis, positioning irisin as a promising therapeutic agent for cardiac injury. AKG ameliorates CTX-induced POI by inhibiting NLRP3-mediated pyroptosis, which provides a new therapeutic strategy and drug target for clinical POI patients.
- | cyclophosphamide / Generic mfg.
Preclinical, Journal: Thiolutin, a selective NLRP3 inflammasome inhibitor, attenuates cyclophosphamide-induced impairment of sperm and fertility in mice. (Pubmed Central) - Mar 25, 2024
THL can improve sperm quality and hormonal balance in OA mice through the inhibition of NLRP3 inflammasome activation. Thus, THL holds promising potential as a therapeutic agent for OA.
- | Preclinical, Journal: Tea polyphenols ameliorates acute lung injury in septic mice by inhibiting NLRP3 inflammasomes (Pubmed Central) - Mar 23, 2024
Thus, THL holds promising potential as a therapeutic agent for OA. TP inhibits NLRP3 inflammasome-associated inflammation to alleviate CLP-induced acute lung injury in mice through a regulatory mechanism that inhibits NOX4 expression and reduces oxidative stress in the lung tissue.
- | chlorogenic acid / Jiuzhang Biotech
Preclinical, Journal: Chlorogenic acid alleviates acute kidney injury in septic mice by inhibiting NLRP3 inflammasomes and the caspase-1 canonical pyroptosis pathway (Pubmed Central) - Mar 23, 2024
TP inhibits NLRP3 inflammasome-associated inflammation to alleviate CLP-induced acute lung injury in mice through a regulatory mechanism that inhibits NOX4 expression and reduces oxidative stress in the lung tissue. CGA alleviates AKI in mice with CLP-induced sepsis by inhibiting NLRP3 inflammasomes and the caspase-1 signaling pathway.
- | Journal: Exploring the therapeutic potential of Anastatica hierochuntica essential oil in DSS-induced colitis. (Pubmed Central) - Mar 23, 2024
In addition, EOAH restored the expression of occludin and ZO-1 proteins in colonic tissues affected by ulcerative colitis (UC). These findings indicate that supplementing with EOAH might offer a novel therapeutic approach for UC prevention.
- | Journal: Xijiao Dihuang decoction combined with Yinqiao powder promotes autophagy-dependent ROS decrease to inhibit ROS/NLRP3/pyroptosis regulation axis in influenza virus infection. (Pubmed Central) - Mar 23, 2024
XDY can promote an intact autophagy flux to eliminate damaged mitochondria, namely mitophagy, which reduces the intracellular ROS accumulation contributing to NLRP3 inflammasome activation, restricting pyroptosis and eventually alleviating the influenza virus-induced inflammatory lesions. The obtained results provide new insights into the mechanism of action of XDY in alleviating influenza virus pneumonia, especially the roles of XDY in anti-oxidation, anti-inflammation and anti-pyroptosis, with potential therapeutic targets for future application in integrative medicine.
- Aryl hydrocarbon receptor confers protection against macrophage pyroptosis and intestinal inflammation through regulating polyamine biosynthesis (Room W176) - Mar 22, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_431;
The obtained results provide new insights into the mechanism of action of XDY in alleviating influenza virus pneumonia, especially the roles of XDY in anti-oxidation, anti-inflammation and anti-pyroptosis, with potential therapeutic targets for future application in integrative medicine. These findings suggest a functional role for the AhR/ODC1/polyamine axis in maintain intestinal homeostasis.
- Blocking of NLRP3 inflammasome activity alleviates iron-induced adverse effects in murine models of colitis (Room W179) - Mar 22, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_405;
Intriguingly, deficiency of NLRP3 in HfeKO mice (Hfe-Nlrp3-DKO) significantly protected them from IL-10R neutralization-induced colitis. In conclusion, our study demonstrates that excess iron could exacerbate inflammation during IBD and that BHB could be used as a therapeutic to mitigate iron-induced inflammation in IBD.
- Air pollution PM2.5 uptake by macrophages induces NLRP3 inflammasome-dependent IL1 (Room W185) - Mar 22, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_359;
In conclusion, our study demonstrates that excess iron could exacerbate inflammation during IBD and that BHB could be used as a therapeutic to mitigate iron-induced inflammation in IBD. Moreover, specific inhibition of superoxide anion production from mitochondrial respiratory Complex I, but not III, blunted IL1
- Loss of myeloid-KLF2 mediates LPS-induced mortality in neonatal pups by NLRP3 inflammasome signaling and altered neutrophil aging (Room W185) - Mar 22, 2024 - Abstract #IMMUNOLOGY2024IMMUNOLOGY_357;
It accelerates neutrophil aging, but leads to persistence of aged neutrophils in the circulation by reducing CXCR4 expression. Future mechanistic studies will focus on KLF2's regulation of NLRP3 and CXCR4 expression at P4 and P12.
- | Journal: Neutrophil extracellular traps induce pyroptosis of pulmonary microvascular endothelial cells by activating the NLRP3 inflammasome. (Pubmed Central) - Mar 22, 2024
Pretreated with the NLRP3 inhibitor MCC950, the activation of NLRP3 inflammasome and pyroptosis of HPMECs were effectively inhibited. Our study confirmed that NETs promote pulmonary microvascular endothelial pyroptosis by activating the NLRP3 inflammasome, suggesting that NETs-induced pyroptosis of PMECs may be a potential pathogenic mechanism of inflammatory exudation in ILD.
- | Journal: VDR and deubiquitination control neuronal oxidative stress and microglial inflammation in Parkinson's disease. (Pubmed Central) - Mar 22, 2024
Importantly, we discovered a novel deubiquitinase DUB3, whose N-terminal catalytic domain interacted with the C-terminal ligand-binding domain of VDR to reduce VDR ubiquitination. Identification of DUB3 as an essential player in the deubiquitinating mechanism of VDR provides valuable insights into VDR regulation and its potential as a therapeutic target for PD.
- | Journal: Lactobacillus Plantarum Promotes Wound Healing by Inhibiting the NLRP3 Inflammasome and Pyroptosis Activation in Diabetic Foot Wounds. (Pubmed Central) - Mar 21, 2024
Our findings uncovered a novel role of LP in diabetic foot wound healing via regulation of the NLRP3 inflammasome, suggesting this link as a therapeutic target. In future research, it would be valuable to explore the signaling cascades involved in LP-mediated inhibition of NLRP3 inflammasome activation.
- | Preclinical, Journal: Folic Acid Rescues Dopaminergic Neurons in MPTP-Induced Mice by Inhibiting the NLRP3 Inflammasome and Ameliorating Mitochondrial Impairment. (Pubmed Central) - Mar 21, 2024
Notable limitations of our study include its reliance on a single animal model and the incompletely elucidated mechanisms underlying the impact of FA on mitochondrial dynamics. Future investigations will explore the clinical utility of FA and its molecular mechanisms, further advancing it as a potential therapeutic for managing and delaying the progression of PD.
- | Journal: Advancements in Predictive Medicine: NLRP3 Inflammasome Inhibitors and AI-Driven Predictive Health Analytics. (Pubmed Central) - Mar 20, 2024
By analyzing complex biomarker data, AI provides crucial insights into individual health trajectories, enabling early interventions and customized treatment plans. This convergence of cutting-edge therapies and AI technology heralds a new era in precision medicine and personalized healthcare strategies.
- | Journal: Vagus nerve stimulation as a promising neuroprotection for ischemic stroke via ?7nAchR-dependent inactivation of microglial NLRP3 inflammasome. (Pubmed Central) - Mar 20, 2024
The role of ?7nAChR in microglial NLRP3 inflammasome activation in ischemic stroke was further validated using genetic manipulations, including Chrna7 knockout mice and microglial Chrna7 overexpression mice, as well as pharmacological interventions using the ?7nAChR inhibitor methyllycaconitine and agonist PNU-282987. Collectively, this study demonstrates the potential of VNS as a safe and effective strategy to treat ischemic stroke, and presents a new approach targeting microglial NLRP3 inflammasome, which might be therapeutic for other inflammation-related diseases.
- | Journal: Tau induces inflammasome activation and microgliosis through acetylating NLRP3. (Pubmed Central) - Mar 19, 2024
Collectively, this study demonstrates the potential of VNS as a safe and effective strategy to treat ischemic stroke, and presents a new approach targeting microglial NLRP3 inflammasome, which might be therapeutic for other inflammation-related diseases. In conclusion, our findings provide evidence for a novel role of Tau in the regulation of microglia activation through acetylating NLRP3, which has potential implications for early intervention and personalised treatment of AD and related Tauopathies.
- | sevoflurane / Generic mfg.
Preclinical, Journal: mtDNA-cGAS-STING axis-dependent NLRP3 inflammasome activation contributes to postoperative cognitive dysfunction induced by sevoflurane in mice. (Pubmed Central) - Mar 18, 2024
Blocking the mtDNA release via the mPTP-VDAC channel inhibitor attenuated sevoflurane-induced mtDNA cytosolic escape and reduced cGAS-STING pathway activation in microglia, finally inhibiting the NLRP3 inflammasome activation. Therefore, regulating neuroinflammation by targeting the cGAS-STING pathway may provide a novel therapeutic target for POCD.
- | Journal: Discovery of anti-inflammatory agents from 3, 4-dihydronaphthalene-1(2H)-one derivatives by inhibiting NLRP3 inflammasome activation. (Pubmed Central) - Mar 18, 2024
Molecular docking analysis confirmed that 7a could reasonably bind the active sites of NLRP3, ASC and p65 proteins. Therefore, 7a is predicted as a potential NLRP3 inflammatory vesicle inhibitor and deserves further research and development.
- | Journal: The discovery of novel and potent indazole NLRP3 inhibitors enabled by DNA-encoded library screening. (Pubmed Central) - Mar 18, 2024
A CADD analysis of the interaction of compound 3 with the NLRP3 NACHT domain proposes a binding site that is distinct from those of ADP and MCC950 and includes specific site interactions. We anticipate that compound 3 (BAL-0028) and other members of this novel indazole class of neutral inhibitors will demonstrate significantly different physical, biochemical, and biological properties compared to NLRP3 inhibitors previously identified.
- || Review, Journal: The research progression of direct NLRP3 inhibitors to treat inflammatory disorders. (Pubmed Central) - Mar 18, 2024
In this review, we provide a summary of direct inhibitors targeting NLRP3, elucidating their inhibitory mechanisms, clinical trial phases, and potential applications. Through this discussion, we aim to shed light on the implications of NLRP3 inhibition for the treatment of inflammatory diseases.
- | Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim
Preclinical, Journal: Empagliflozin ameliorates vascular calcification in diabetic mice through inhibiting Bhlhe40-dependent NLRP3 inflammasome activation. (Pubmed Central) - Mar 18, 2024
We conclude that EMPA ameliorates VC by inhibiting Bhlhe40-dpendent NLRP3 inflammasome activation. These results might provide potential significance for EMPA in VC therapy of T2DM patients.