NLRP3 inhib 
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  • ||||||||||  Journal:  Protective effects of propofol on experimental neonatal acute lung injury. (Pubmed Central) -  Aug 1, 2019   
    Furthermore, LPS induced the upregulation of phosphorylated (p‑)p38, nuclear factor κ‑light‑chain‑enhancer of activated B cells (NF‑κB), p‑p65, NLR family pyrin domain containing 3 (NLRP3), apoptosis‑associated speck‑like protein containing CARD and caspase‑1 in lung tissues of neonatal rats, and treatment with propofol was able to downregulate these factors in a dose‑dependent manner. Propofol alleviated lung injury in neonatal rats with LPS‑induced ALI by preventing inflammation and oxidative stress via the regulation of the activity of the p38 mitogen‑activated protein kinase/NF‑κB signaling pathway and the expression levels of the NLRP3 inflammasome.
  • ||||||||||  Journal:  MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition. (Pubmed Central) -  Jul 31, 2019   
    MCC950 is a potent and specific small-molecule inhibitor of the NLRP3 pathway, but its molecular target is not defined. Here, we show that MCC950 directly interacts with the Walker B motif within the NLRP3 NACHT domain, thereby blocking ATP hydrolysis and inhibiting NLRP3 activation and inflammasome formation.
  • ||||||||||  Journal:  MCC950 closes the active conformation of NLRP3 to an inactive state. (Pubmed Central) -  Jul 31, 2019   
    However, the mechanism of action of MCC950 remains unknown. Here, we characterize the mechanism of action of MCC950 in both wild-type and autoinflammatory-related NLRP3 mutants, and demonstrate that MCC950 closes the 'open' conformation of active NLRP3.
  • ||||||||||  Journal:  STUDY ON THE INFLAMMASOME NLRP3 AND BLIMP-1/NLRP12 AFTER KERATINOCYTE EXPOSURE TO CONTACT ALLERGENS. (Pubmed Central) -  Jul 31, 2019   
    By immunohistochemistry, we found increased NLRP3 expression following exposure to contact allergens, and observed a nuclear co-localization of the two proteins, indicating the NLRP12 likely acts preventing the cytosolic localization of NLRP3 and inflammasome assembly. Finally, contact allergen-induced Blimp-1 mRNA and protein expression can be completely blocked by inhibiting NF-κB activation, confirming the central role of NF-κB in contact allergen-induced keratinocyte activation.
  • ||||||||||  Journal:  Epac1 inhibits PKR to reduce NLRP3 inflammasome proteins in retinal endothelial cells. (Pubmed Central) -  Jul 31, 2019   
    Furthermore, despite the addition of recombinant human PKR, Epac1 was still able to significantly reduce NLRP3 signaling. Overall, these studies demonstrated that PKR regulates the NLRP3 inflammasome in REC, and that Epac1 inhibition of PKR can reduce activation of the NLRP3 inflammasome.
  • ||||||||||  doxorubicin hydrochloride / generics
    Journal:  Trimethylamine N-Oxide Exacerbates Cardiac Fibrosis via Activating the NLRP3 Inflammasome. (Pubmed Central) -  Jul 31, 2019   
    ...Methods and To determine the role of TMAO-mediated cardiac fibrosis, we established mouse models of doxorubicin (DOX)-induced cardiac fibrosis with or without TMAO in drinking water...Importantly, the silencing of NLRP3 presented a protection effect against cardiac fibrosis including cellular proliferation, migration and collagen deposition in vitro. Our data suggested that TMAO aggravated DOX-induced mouse cardiac fibrosis, at least in part, through activation of the NLRP3 inflammasome, providing a new potential target for preventing the progression of cardiac fibrosis.
  • ||||||||||  Journal:  A Role for the Inflammasome in Spontaneous Labor at Term. (Pubmed Central) -  Jul 28, 2019   
    Spontaneous labor at term is characterized by the expression of inflammasome components, which may participate in the activation of caspase-1 and lead to the cleavage and release of mature IL-1β by the chorioamniotic membranes. These results support the participation of the inflammasome in the mechanisms responsible for spontaneous parturition at term.
  • ||||||||||  Clinical, Review, Journal:  Salvia miltiorrhiza in diabetes: A review of its pharmacology, phytochemistry, and safety. (Pubmed Central) -  Jul 28, 2019   
    SM may offer a new strategy for prevention and treatment of diabetes and its complications that stimulates extensive research into identifying potential anti-diabetic compounds and fractions as well as exploring the underlying mechanisms of this herb. Further scientific evidences are still required from well-designed preclinical experiments and clinical trials on its anti-diabetic effects and safety.
  • ||||||||||  Preclinical, Journal:  Estrogen ameliorates allergic airway inflammation via regulating the activation of NLRP3 inflammasome in mice. (Pubmed Central) -  Jul 26, 2019   
    Furthermore, E2 suppressed both the messenger ribonucleic acid (mRNA) expression and protein expression of NLRP3, caspase-1 and IL-1β. In summary, our study showed that NLRP3 inflammasome activation and pro-inflammatory cytokine production markedly increased in OVA-induced airway inflammation, and E2 effectively abrogated such inflammation by regulating the activation of NLRP3.
  • ||||||||||  Byetta (exenatide) / AstraZeneca
    Preclinical, Journal, IO Biomarker:  Renal effects of exendin-4 in an animal model of brain death. (Pubmed Central) -  Jul 26, 2019   
    Nlrp3 and Tnf expressions were up-regulated in the BD group compared with controls, but Ex-4 treatment had no effect on these genes. Our findings suggest that Ex-4 administration in BD rats reduces BD-induced kidney damage by decreasing the expression of oxidative stress genes and increasing the expression of Bcl2.
  • ||||||||||  Journal:  Inflammation: Specific inhibition of NLRP3 comes closer. (Pubmed Central) -  Jul 26, 2019   
    Our findings suggest that Ex-4 administration in BD rats reduces BD-induced kidney damage by decreasing the expression of oxidative stress genes and increasing the expression of Bcl2. No abstract available
  • ||||||||||  Clinical, Journal:  Uric acid and the vaccine adjuvant activity of aluminum (oxy)hydroxide nanoparticles. (Pubmed Central) -  Jul 26, 2019   
    The aluminum (oxy)hydroxide nanoparticles' ability to stimulate uric acid production was also confirmed in cell culture. We concluded that the stronger adjuvant activity of insoluble aluminum (oxy)hydroxide nanoparticles, relative to microparticles, may be attributed at least in part to their stronger ability to induce endogenous danger signals such as uric acid.
  • ||||||||||  galantamine hydrobromide / generics
    Preclinical, Journal:  Acceleration of NLRP3 inflammasome by chronic cerebral hypoperfusion in Alzheimer's disease model mouse. (Pubmed Central) -  Jul 26, 2019   
    These pathological changes were ameliorated by galantamine treatment. The present study demonstrated that CCH strongly enhanced primary AD pathology including neuroinflammation, Aβ accumulations and NVU dissociation in AD mice, which was greatly protected by an allosterically potentiating ligand galantamine.
  • ||||||||||  Journal:  Self-assembled hyaluronic acid nanoparticles: Implications as a nanomedicine for treatment of type 2 diabetes. (Pubmed Central) -  Jul 24, 2019   
    Interestingly, treatment with HA-NPs in DIO mice suppressed adipose tissue inflammation as indicated by reduced macrophage content, the production of proinflammatory cytokines and NLRP3 inflammasome activity in eWATs, leading to improved insulin sensitivity and normalized blood glucose levels. Collectively, these results suggest that an empty HA-NP itself can be a therapeutic agent for the treatment of type 2 diabetes.
  • ||||||||||  Journal:  Cutting Edge: The Heat Shock Protein gp96 Activates Inflammasome-Signaling Platforms in APCs. (Pubmed Central) -  Jul 24, 2019   
    This is shown to initiate inflammatory conditions in vivo in the absence of additional known inflammasome activators or infection. These results document a novel mechanism by which proteins of endogenous origin, the HSPs, can modulate an inflammatory response following their release from aberrant cells.
  • ||||||||||  Bay11-7082 / InvivoGen
    Journal:  Astragaloside IV Suppresses High Glucose-Induced NLRP3 Inflammasome Activation by Inhibiting TLR4/NF-κB and CaSR. (Pubmed Central) -  Jul 24, 2019   
    In addition, both NPS2143 and BAY 11-7082 attenuated high glucose-induced upregulation of NLRP3, ASC, caspase-1, IL-18, and IL-1β expression. In conclusion, this study suggested that As-IV could inhibit high glucose-induced NLRP3 inflammasome activation and subsequent secretion of proinflammatory cytokines via inhibiting TLR4/NF-κB signaling pathway and CaSR, which provides new insights into the anti-inflammatory activity of As-IV.
  • ||||||||||  Journal:  NLRP3 Inflammasome Is Involved in Calcium-Sensing Receptor-Induced Aortic Remodeling in SHRs. (Pubmed Central) -  Jul 24, 2019   
    In vascular smooth muscle cells (VSMCs), the activation of NLRP3 inflammasome associated with CaSR and collagen synthesis was induced by angiotensin II (Ang II). Furthermore, inhibition of CaSR and NLRP3 inflammasome attenuated proinflammatory cytokine release, suggesting that CaSR-mediated activation of the NLRP3 inflammasome may be a therapeutic target in aortic dysfunction and vascular inflammatory lesions.
  • ||||||||||  Preclinical, Journal:  Effects of GBE50 on LPS/ATP induced NLRP3 inflammasome activation in primary rat microglia (Pubmed Central) -  Jul 21, 2019   
    GBE50 (10 mg·L⁻¹) preconditioning could significantly inhibit the expression of LPS (100 μg·L⁻¹,12 h), ATP (5 mmol·L⁻¹, 30 min) induced primary microglia corpuscle associated protein, inflammatory corpuscle aggregation, and the release of inflammatory factors IL-6 and TNF-α. These results indicated that GBE50 could inhibit the secretion of inflammatory factors after microglia activation, which is related to down regulating the protein expression and activity of NLRP3 inflammatory corpuscle.
  • ||||||||||  Journal:  Mechanisms of Inflammasome Signaling, microRNA Induction and Resolution of Inflammation by Helicobacter pylori. (Pubmed Central) -  Jul 21, 2019   
    In this chapter, we will pinpoint the role of H. pylori in TLR- and NLRP3 inflammasome-dependent signaling together with the differential functions of pro- and anti-inflammatory cytokines. Moreover, the impact of microRNAs on H. pylori-host interaction will be discussed, and its role in resolution of infection versus chronic infection, as well as in gastric disease development.
  • ||||||||||  Journal:  Variants in NLRP3 and NLRC4 inflammasome associate with susceptibility and severity of multiple sclerosis. (Pubmed Central) -  Jul 19, 2019   
    This intronic polymorphism have been previously associated to decreased NLRC4 transcription and low IL-18 serum level, indicated once more that less activation of inflammasome and IL-18 production are beneficial for MS patients. PBM analysis showed that MS cells express higher level of inflammasome genes than HD ones, and are more prone to respond to a classical NLRP3 stimulus than HD.
  • ||||||||||  Clinical, Journal:  Correlation Between the NLRP3 Inflammasome and the Prognosis of Patients With LSCC. (Pubmed Central) -  Jul 18, 2019   
    The high expression group of the NLRP3 inflammasome (NLRP3/IL-18/IL-1β/ASC) had a poorer prognosis (OS and DFS) than the low expression group of LSCC patients 5 years after surgery. The NLRP3 inflammasome (NLRP3/IL-18/IL-1β/ASC) may be used as an auxiliary indicator to predict LSCC patient prognosis after surgery.