- |||||||||| belnacasan (VX-765) / Vertex, Tudcabil (tauroursodeoxycholic acid) / Bruschettini
Journal: Endoplasmic Reticulum Stress Mediated NLRP3 Inflammasome Activation and Pyroptosis in THP-1 Macrophages Infected with Bacillus Calmette-Gu (Pubmed Central) - Aug 2, 2023 Compared with specific Caspase-1 inhibitor VX-765, pan-Caspase inhibitor Z-VAD-FMK showed a more significant inhibitory effect on BCG infection-induced pyroptosis of THP-1 macrophages. Taken together, this study demonstrates that ERS mediated NLRP3 inflammasome activation and pyroptosis after BCG infection of THP-1 macrophages, and that BCG infection of THP-1 macrophages induces pyroptosis through canonical and noncanonical pathways.
- |||||||||| Zyclara (imiquimod) / Mochida, Viatris, Bausch Health
Preclinical, Journal: Evidence on the therapeutic role of thiolutin in imiquimod-induced psoriasis-like skin inflammation in mice. (Pubmed Central) - Aug 1, 2023 Taken together, this study demonstrates that ERS mediated NLRP3 inflammasome activation and pyroptosis after BCG infection of THP-1 macrophages, and that BCG infection of THP-1 macrophages induces pyroptosis through canonical and noncanonical pathways. THL may alleviate IMQ-induced psoriasis-like manifestations in mice by inhibiting NLRP3 inflammasome.
- |||||||||| Journal: Ginsenoside compound K alleviates osteoarthritis by inhibiting NLRP3?mediated pyroptosis. (Pubmed Central) - Jul 31, 2023
Immunohistochemistry staining of the knee joint tissue sections from the DMM mice confirmed that GCK attenuated the NLRP3 and GSDMD-NT expression that was induced by DMM surgery. In conclusion, the present study revealed that GCK can reduce cartilage degradation in an osteoarthritis model by inhibiting the NLRP3-inflammasome activation and subsequent pyroptosis.
- |||||||||| Journal: Atranorin inhibits NLRP3 inflammasome activation by targeting ASC and protects NLRP3 inflammasome-driven diseases. (Pubmed Central) - Jul 31, 2023
Moreover, Atranorin ameliorates intestinal inflammation and epithelial barrier dysfunction in DSS induced mice ulcerative colitis and inhibits NLRP3 inflammasome activation in colon. Altogether, our study identifies Atranorin as a novel NLRP3 inhibitor that targets ASC protein and highlights the potential therapeutic effects of Atranorin in NLRP3 inflammasome-driven diseases including acute inflammation, gouty arthritis and ulcerative colitis.
- |||||||||| Journal: TWEAK promotes inflammatory response in liver fibrosis. (Pubmed Central) - Jul 28, 2023
According to our results, TWEAK promoted M1 polarization of liver KCs and J774A.1 cells, and silencing CD266 expression or treatment with the NLRP3 inhibitor suppressed the effect of TWEAK. In the mouse experiment, it was discovered that after knocking down NLRP3 expression or using NLRP3 inhibitor to antagonize the effect of TWEAK, the mouse liver function and M1 cell level in liver tissues were improved.
- |||||||||| Journal: Loganin alleviates myocardial ischemia-reperfusion injury through GLP-1R/NLRP3-mediated pyroptosis pathway. (Pubmed Central) - Jul 27, 2023
GLP-1R/NLRP3 activation by GLP-1R inhibition or NLRP3 overexpression reversed the suppressive effects of loganin on OGD/R-induced cardiomyocyte pyroptosis. These data indicated that loganin prevented OGD/R-induced proliferation inhibition, apoptosis and pyroptosis in OGD/R-treated cardiomyocytes by inhibiting GLP-1R/NLRP3 activity, indicating the therapeutic potential of loganin in myocardial I/R injury.
- |||||||||| glibenclamide / Generic mfg., dimethyl fumarate / Generic mfg.
Preclinical, Journal: Dimethyl fumarate-mediated Nrf2/ARE pathway activation and glibenclamide-mediated NLRP3 inflammasome cascade inhibition alleviate type II diabetes-associated fatty liver in rats by mitigating oxidative stress and inflammation. (Pubmed Central) - Jul 21, 2023 (IL-1?), nuclear factor-?B (NF-?B), Nrf2, superoxide dismutase 1, catalase, IGF 1, heme oxygenase 1, receptor for the advanced glycation end product (RAGE), and collagen-1 in diabetic rats. Further, a mechanistic molecular study employing other specific NLRP3 inhibitors and Nrf2 activators will significantly contribute to the development of novel therapy for fatty liver diseases.
- |||||||||| Review, Journal: A Patent Review of NLRP3 Inhibitors to Treat Autoimmune Diseases. (Pubmed Central) - Jul 20, 2023
Due to the complex nature of the NLRP3 inflammasome, novel screening assays along with target engagement methods could benefit the drug discovery and clinical translation. In addition, clinical trials on NLRP3 inhibitors are still in their early stages, and continuous investigations are needed to fully assess their safety and effectiveness.
- |||||||||| Legalon (silibinin) / Viatris
Review, Journal: Beneficial effects of flavonoids on cardiovascular diseases by influencing NLRP3 inflammasome. (Pubmed Central) - Jul 19, 2023 In brief, the PDB format of NLRP3 was selected as a protein file, and 34 flavonoids in SDF format were selected as the ligand file, and then input to CB-Dock for molecular docking. The docking results showed that epigallocatechin-3-gallate (EGCG), amentoflavone, baicalin, scutellarin, vitexin, silibinin, and puerarin had good binding affinities to NLRP3, which could be used as NLRP3 inhibitors, and aid in the discovery of lead compounds for the design and development of CVDs.
- |||||||||| Journal: FoxO1/NLRP3 Inflammasome Promotes Age-Related Alveolar Bone Resorption. (Pubmed Central) - Jul 14, 2023
Concordant with our study, MCC950, a specific inhibitor of NLRP3 inflammasome, greatly rescued osteoblast differentiation under oxidative stress. Our data shed light on the manifestations of FoxO1 depletion in osteoblasts and propose a possible mechanism for the therapy of age-related alveolar bone loss.
- |||||||||| Review, Journal: NLRP3 inflammasome activation after ischemic stroke. (Pubmed Central) - Jul 12, 2023
In addition, we go over how pyroptosis interacts with other processes for regulated cell death. In addition, specific NLRP3 inflammasome pathway inhibitors are identified, which offer new approaches to preventing ischemic brain injury.
- |||||||||| Journal: Molecular mechanism of miRNA-23a in sepsis-induced lung injury. (Pubmed Central) - Jul 12, 2023
In addition, specific NLRP3 inflammasome pathway inhibitors are identified, which offer new approaches to preventing ischemic brain injury. miR-23a can significantly alleviate sepsis-induced lung injury in CLP-induced septic mice and LPS-stimulated cell lines by suppressing NLRP3 inflammasome activation and inflammatory response, while promoting the CXCR4/PTEN/PI3K/AKT pathway.
- |||||||||| Journal: Encapsulation of MCC950 in Liposomes Decorated with Anti-Frizzled 1 Improves Drug Bioavailability and Effectiveness in Fatty Liver Disease. (Pubmed Central) - Jul 7, 2023
Luminescent carbon dots (CDs) were also co-encapsulated with MCC950 in LPs to obtain optically traceable nanoformulations that have proved the enhanced ability of the targeted LPs to be internalized into THP-1 cells with respect to their nontargeted counterparts. Our results suggest that MCC950 encapsulation into targeted LPs represents a valuable strategy to achieve reformulation of the NLRP3 inhibitor, able to significantly curtail the threshold of MCC950 doses for inhibiting inflammasome activation, thus offering a new therapeutic approach.
- |||||||||| C9orf72 dipeptides trigger neuroinflammation via the NLRP3 inflammasome (In-Person) - Jul 6, 2023 - Abstract #AAIC2023AAIC_6215;
Here, we demonstrate that C9orf72 dipeptides could directly contribute to neuroinflammation in FTD/ALS via the NLRP3 inflammasome. Furthermore, we demonstrate that this can be inhibited pharmacologically, highlighting NLRP3 as a potential therapeutic target in FTD/ALS.
- |||||||||| Development of NLRP3 PET Radiotracers for Alzheimer's disease (In-Person) - Jul 6, 2023 - Abstract #AAIC2023AAIC_2018;
Modulation of purinergic signalling has the potential to regulate neuroinflammation and the ability of P2X7 receptor antagonists to suppress a pro-inflammatory response by microglia suggests this pharmacological action may offer benefit to patients with AD. A novel C-11 labeled NRP3 PET radiotracer was developed and demonstrated to serve as a suitable CNS PET tracer to monitor inflammatory responses in the brain.
- |||||||||| Journal: Unified Total Synthesis of the Limonoid Alkaloids: Strategies for the De Novo Synthesis of Highly Substituted Pyridine Scaffolds. (Pubmed Central) - Jul 3, 2023
In addition, NMR calculations suggested structural misassignment of several limonoid alkaloids, and predicted their C3-epimers as the correct structures, which was further validated unequivocally through chemical synthesis. The materials produced in this study were evaluated for cytotoxicity, anti-oxidant effects, anti-inflammatory action, PTP1B and Nlrp3 inflammasome inhibition, which led to compelling anti-inflammatory activity and anti-oxidant effects being discovered.
- |||||||||| Journal: MARCH9 Mediates NOX2 Ubiquitination to Alleviate NLRP3 Inflammasome-Dependent Pancreatic Cell Pyroptosis in Acute Pancreatitis. (Pubmed Central) - Jul 2, 2023
The materials produced in this study were evaluated for cytotoxicity, anti-oxidant effects, anti-inflammatory action, PTP1B and Nlrp3 inflammasome inhibition, which led to compelling anti-inflammatory activity and anti-oxidant effects being discovered. Our results suggested that MARCH9 suppresses NLRP3 inflammasome-mediated pancreatic cell injury through mediating the ubiquitination and degradation of NADPH oxidase-2, which compromises ROS generation and NLRP3 inflammasomal activation.
- |||||||||| Journal: The landscape of mitophagy in sepsis reveals PHB1 as an NLRP3 inflammasome inhibitor. (Pubmed Central) - Jun 30, 2023
In addition, mitophagy inhibitor treatment abolished PHB1 knockdown-mediated activation of NLRP3 inflammasomes, suggesting that PHB1 inhibited the activation of inflammasomes through mitophagy. In conclusion, this study reveals that a high degree of mitophagy may predict a good outcome of sepsis, and PHB1 is a key NLRP3 inflammasome regulator via mitophagy in inflammatory diseases such as sepsis.
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